| 产品标题 |
产品货号 |
产品规格 |
厂家 |
| GMC 2-113 | Axon 1083
CAS [256227-77-7]
MF C28H29N5O3MW 483.56
Purity:
98%
Soluble in 0.1N HCl(aq) and DMSO
Description
Selective 5-HT1B antagonist; ratio of IC50 affinities for 1B vs 1D up to 63
References
Certificates
Categories
Extra info
Y Liao et al. New selective and potent 5-HT1B/1D or 5-HT1B antagonists: chemistry and pharmacological evaluation of GR127935-like compounds. J. Med. Chem. 2000, 43, 517-525.
JW Clitherow et al. Evolution of a novel series of [(N,N-dimethylamino)propyl]- and piperazinylbenzalides as the first selective 5-HT1D antagonists. J. Med. Chem. 1994, 37, 2253.
Certificate of Analysis
Material Safety Data Sheet
CNS
5-HT1B
A19
5-HT1B antagonist
Chemical name
2'-Methyl-4'-(5-methyl-[1,3,4]oxadiazol-2-yl)-biphenyl-4-carboxylic acid [4-hydroxy-3-(4-methyl-piperazin-1-yl)-phenyl]-amide
Parent CAS No.
[256227-77-7]
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Size
Unit Price
Stock
10 mg
€155.00
In Stock | | axonmedchem |
| CP 94253 hydrochloride | Axon 1945
CAS [845861-39-4]
MF C15H19N3O.HClMW 293.79
Purity:
99%
Soluble in water and DMSO
Description
Potent and selective serotonin 5-HT1B receptor agonist, with Ki values to be 2 nM for 5-HT1B and 89, 860, 49 and 1600 nM for 5-HT1A, 5-HT1C, 5-HT1D and 5-HT2 receptors respectively
References
Certificates
Categories
Extra info
KB Koe et al. Biochemical and behavioral studies of the 5-HT1B receptor agonist, CP-94,253. Drug Devel. Res. 1992, 26(3), 241-250.
MD Lee, KJ Simansky. CP-94,253: a selective serotonin1B (5-HT1B) agonist that promotes satiety. Psychopharmacol. 1997, 131 (3), 264-270.
E Tatarczyńska et al. Antidepressant-like effect of the selective 5-HT1B receptor agonist CP 94253: a possible mechanism of action. Eur. J. Pharmacol. 2005, 516(1), 46-50.
Certificate of Analysis
Material Safety Data Sheet
CNS
5-HT1B
A19
Potent and selective serotonin 5-HT1B receptor agonist
Chemical name
5-propoxy-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-pyrrolo[3,2-b]pyridine hydrochloride
Parent CAS No.
[131084-35-0]
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Size
Unit Price
Stock
10 mg
€105.00
In Stock | | axonmedchem |
| GR 127935 hydrochloride | Axon 1813
CAS [148642-42-6]
MF C29H31N5O3.HClMW 534.05
Purity:
99%
Soluble in water and DMSO
Description
Putative and selective 5-HT1B/1D antagonist
References
Certificates
Categories
Extra info
PJ Pauwels. Pharmacological Properties of a Putative 5-HT1B/D Receptor Antagonist GR 127,935. CNS Drug Reviews 1996, 2(4), 415–428.
JW Clitherow et al. Evolution of a novel series of [(N,N-dimethylamino)propyl]- and piperazinylbenzalides as the first selective 5-HT1D antagonists. J. Med. Chem. 1994, 37, 2253.
Y Liao et al. New selective and potent 5-HT1B/1D or 5-HT1B antagonists: chemistry and pharmacological evaluation of GR127935-like compounds. J. Med. Chem. 2000, 43, 517-525.
Certificate of Analysis
Material Safety Data Sheet
CNS
5-HT1B
5-HT1D
A19
5-HT1B and 5-HT1D antagonist
Chemical name
N-(4-methoxy-3-(4-methylpiperazin-1-yl)phenyl)-2'-methyl-4'-(5-methyl-1,2,4-oxadiazol-3-yl)biphenyl-4-carboxamide hydrochloride
Parent CAS No.
[148672-13-3]
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Size
Unit Price
Stock
10 mg
€135.00
In Stock | | axonmedchem |
| Sumatriptan succinate - GR 43175 | GW 102 | SN 308 | Axon 1352
CAS [103628-48-4]
MF C14H21N3O2S.C4H6O4MW 413.49
Purity:
99%
Soluble in DMSO
Description
Selective 5-HT1B/1D receptor agonist indicated for the treatment of migraine headaches
References
Certificates
Categories
Extra info
Sumatriptan. WHO Drug Information 1988, 2(2), 111.
C De Battista and K Mueller. Sumatriptan prophylaxis for postelectroconvulsive therapy headaches. Headache 1995, 35(8), 502-503.
Z Razzaque et al. Vasoconstriction in human isolated middle meningeal arteries: determining the contribution of 5-HT1B- and 5-HT1F-receptor activation. Br J Clin Pharmacol 1999, 47(1), 75–82.
Certificate of Analysis
Material Safety Data Sheet
CNS
5-HT1B
5-HT1D
A19
5-HT1B and 5-HT1D agonist
Chemical name
1-{3-[2-(dimethylamino)ethyl]-1H-indol-5-yl}-N-methylmethanesulfonamide succinate
Parent CAS No.
[103628-46-2]
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Size
Unit Price
Stock
10 mg
€85.00
In Stock | | axonmedchem |
| CGS 12066B | Axon 1206
CAS [109028-10-6]
MF C17H17F3N4.2C4H4O4MW 566.48
Purity:
99%
Soluble in DMSO
Description
Selective serotonin 5-HT1B receptor agonist
References
Certificates
Categories
Extra info
RF Neale et al. Biochemical and pharmacological characterization of CGS 12066B, a selective serotonin-1B agonist. Eur. J. Pharmacol. 1987, 136, 1.
Certificate of Analysis
Material Safety Data Sheet
CNS
5-HT1B
A19
5-HT1B agonist
Chemical name
4-(4-Methyl-piperazin-1-yl)-7-trifluoromethyl-pyrrolo[1,2-a]quinoxaline dimaleate
Parent CAS No.
[109028-09-3]
Order
Size
Unit Price
Stock
10 mg
€75.00
In Stock | | axonmedchem |
| CP 135807 | Axon 2102
CAS [151272-90-1]
MF C19H21N5O2MW 351.40
Purity:
99%
Optical purity:
Optically pure
Soluble in DMSO
Description
Selective 5-HT agonist which binds with high affinity to central 5-HT1D receptors. In functional studies CP 135807 produces dose-dependent decreases in extracellular serotonin
References
Certificates
Categories
Extra info
RS Mansbach et al. CP-135,807, a selective 5-HT1D agonist: effects in drug discrimination and punishment procedures in the pigeon. Psychopharm. (Berl). 1996, 128(3), 313-319.
H Rollema et al. Combined administration of a 5-hydroxytryptamine (5-HT)1D antagonist and a 5-HT reuptake inhibitor synergistically increases 5-HT release in guinea pig hypothalamus in vivo. J. Neurochem. 1996, 67(5), 2204-2207.
Certificate of Analysis
Material Safety Data Sheet
CNS
5-HT1D
A19
Pfizer Licensed Products
Selective 5-HT1D receptor agonist
Chemical name
(R)-3-((1-methylpyrrolidin-2-yl)methyl)-N-(3-nitropyridin-2-yl)-1H-indol-5-amine
Source information
Pfizer compound; Sold for research purposes under agreement from Pfizer Inc.
Parent CAS No.
[151272-90-1]
Order
Size
Unit Price
Stock
5 mg
€75.00
In Stock | | axonmedchem |
| SB 216641 hydrochloride | Axon 1085
CAS [193611-67-5]
MF C28H30N4O4.HClMW 523.02
Purity:
99%
Soluble in water
Description
Selective human 5-HT1B antagonist
References
Certificates
Categories
Extra info
Schlicker et al. Effects of selective h5-HT1B (SB-216641) and 5-HT1D (BRL-15572) receptor ligands on guinea pig and human 5-HT auto- and heteroreceptors. Naunyn-Schmied. Arch. Pharmacol. 1997, 356, 321.
Certificate of Analysis
Material Safety Data Sheet
CNS
5-HT1B
A19
5-HT1B antagonist
Chemical name
2'-Methyl-4'-(5-methyl-[1,2,4]oxadiazol-3-yl)-biphenyl-4-carboxylic acid [3-(2-dimethylamino-ethoxy)-4-methoxy-phenyl]-amide hydrochloride
Parent CAS No.
[170230-39-4]
Order
Size
Unit Price
Stock
10 mg
€135.00
In Stock | | axonmedchem |
| GMC 3-15 | Axon 1081
CAS [691846-63-6]
MF C27H30N4O3MW 458.55
Purity:
99%
Soluble in DMSO
Description
Very potent and selective 5-HT1B/1D antagonist
References
Certificates
Categories
Extra info
Y Liao et al. New selective and potent 5-HT1B/1D or 5-HT1B antagonists: chemistry and pharmacological evaluation of GR127935-like compounds. J. Med. Chem. 2000, 43, 517-525.
JW Clitherow et al. Evolution of a novel series of [(N,N-dimethylamino)propyl]- and piperazinylbenzalides as the first selective 5-HT1D antagonists. J. Med. Chem. 1994, 37, 2253.
Certificate of Analysis
Material Safety Data Sheet
CNS
5-HT1B
5-HT1D
A19
5-HT1B and 5-HT1D antagonist
Chemical name
2-Methyl-biphenyl-4,4'-dicarboxylic acid 4-amide 4'-{[4-methoxy-3-(4-methyl-piperazin-1-yl)-phenyl]-amide}
Parent CAS No.
[691846-63-6]
Order
Size
Unit Price
Stock
10 mg
€145.00
In Stock | | axonmedchem |
| GMC 15-27 | Axon 1082
CAS [256227-71-1]
MF C27H31N5O2MW 457.57
Purity:
98%
No solubility data
Description
Selective 5-HT1B/1D antagonist; most potent in collection
References
Certificates
Categories
Extra info
Y Liao et al. New selective and potent 5-HT1B/1D or 5-HT1B antagonists: chemistry and pharmacological evaluation of GR127935-like compounds. J. Med. Chem. 2000, 43, 517-525.
JW Clitherow et al. Evolution of a novel series of [(N,N-dimethylamino)propyl]- and piperazinylbenzalides as the first selective 5-HT1D antagonists. J. Med. Chem. 1994, 37, 2253.
Certificate of Analysis
Material Safety Data Sheet
CNS
5-HT1B
5-HT1D
A19
5-HT1B and 5-HT1D antagonist
Chemical name
4'-Carbamimidoyl-2'-methyl-biphenyl-4-carboxylic acid [4-methoxy-3-(4-methyl-piperazin-1-yl)-phenyl]-amide
Parent CAS No.
[256227-71-1]
Order
Size
Unit Price
Stock
10 mg
€165.00
In Stock | | axonmedchem |
| GMC 2-29 | Axon 1080
CAS [148672-15-5]
MF C29H31N5O3MW 497.59
Purity:
99%
Soluble in DMSO
Description
Selective 5-HT1B/1D antagonist; GR 127935-like drug with even greater potency in function assays
References
Certificates
Categories
Extra info
Y Liao et al. New selective and potent 5-HT1B/1D or 5-HT1B antagonists: chemistry and pharmacological evaluation of GR127935-like compounds. J. Med. Chem. 2000, 43, 517-525.
JW Clitherow et al. Evolution of a novel series of [(N,N-dimethylamino)propyl]- and piperazinylbenzalides as the first selective 5-HT1D antagonists. J. Med. Chem. 1994, 37, 2253.
Certificate of Analysis
Material Safety Data Sheet
CNS
5-HT1B
5-HT1D
A19
5-HT1B and 5-HT1D antagonist
Chemical name
2'-Methyl-4'-(5-methyl-[1,3,4]oxadiazol-2-yl)-biphenyl-4-carboxylic acid [4-methoxy-3-(4-methyl-piperazin-1-yl)-phenyl]-amide
Parent CAS No.
[148672-15-5]
Order
Size
Unit Price
Stock
10 mg
€145.00
In Stock | | axonmedchem |
| MK 212 hydrochloride | Axon 1214
CAS [67250-10-6]
MF C8H11ClN4.HClMW 235.11
Purity:
99%
No solubility data
Description
5-HT2C receptor agonist
References
Certificates
Categories
Extra info
EA Walker et al. Selective and nonselective serotonin antagonists block the aversive stimulus properties of MK212 and m-chlorophenylpiperazine (mCPP) in mice. Neuropharmacology. 2005, 49(8), 1210-1219.
Certificate of Analysis
Material Safety Data Sheet
CNS
5-HT2C
A17
5-HT2C agonist
Chemical name
6'-Chloro-3,4,5,6-tetrahydro-2H-[1,2']bipyrazinyl hydrochloride
Parent CAS No.
[64022-27-1]
Order
Size
Unit Price
Stock
10 mg
€75.00
In Stock | | axonmedchem |
| Eltoprazine hydrochloride - DU 28853 | Axon 1142
CAS [98206-09-8]
MF C12H16N2O2.HClMW 256.73
Purity:
99%
Soluble in water and DMSO
Description
5-HT1A/1B agonist and 5-HT2C receptor antagonist. Following L-DOPA challenge, Eltoprazine causes a significant reduction of L-DOPA-induced dyskinesias.
References
Certificates
Categories
Extra info
G Griebel et al. Serenics fluprazine (DU 27716) and eltoprazine (DU 28853) enhance neophobic and emotional behaviour in mice. Psychopharmacology 1990, 102, 498-502.
DR. Cherek et al. Acute effects of eltoprazine on aggression and point-mantained responding of normal male participants: Phase I study. Exp. Clin. Psychopharmacol. 1995, 3/3, 287-293.
P. Svenningsson et al. Eltoprazine counteracts l-DOPA-induced dyskinesias in Parkinson's disease: a dose-finding study. Brain. 2015 Feb 10. pii: awu409. [Epub ahead of print]
Certificate of Analysis
Material Safety Data Sheet
CNS
5-HT1A
5-HT1B
5-HT2C
A19
5-HT1A and 5-HT1B agonist
Chemical name
1-(2,3-Dihydro-benzo[1,4]dioxin-5-yl)-piperazine hydrochloride
Parent CAS No.
[98224-03-4]
Order
Size
Unit Price
Stock
10 mg
€82.00
In Stock | | axonmedchem |
| Mirtazapine - Mianserin, 6-Aza- | ORG 3770 | Axon 1138
CAS [85650-52-8]
MF C17H19N3MW 265.35
Purity:
99%
No solubility data
Description
A noradrenergic and specific serotonergic antidepressant (NaSSA); antagonizes selective adrenergic and serotonergic receptors so that both NE release and 5-HT1A mediated serotonergic signaling are increased
References
Certificates
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Extra info
PK Gillman. A systematic review of the serotonergic effects of mirtazapine: implications for its dual action status. Human Psychopharmacol. Clin. Exper. 2006, 21(2), 117-25.
Certificate of Analysis
Material Safety Data Sheet
CNS
5-HT1A
5-HT2C
Adrenoceptor α2
H1
A17
5-HT antidepressant
Chemical name
2-Methyl-1,2,3,4,9,13b-hexahydro-2,4a,5-triaza-tribenzo[a,c,e]cycloheptene
Parent CAS No.
[85650-52-8]
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Size
Unit Price
Stock
10 mg
€65.00
In Stock | | axonmedchem |
| RO 60-0175 | Axon 1118
CAS [169675-09-6]
MF C11H12ClFN2.C4H4O4MW 342.75
Purity:
99%
Optical purity:
>98% ee
Soluble in DMSO
Description
Putative 5-HT2C agonist; selectivity on 2C is under argument
References
Certificates
Categories
Extra info
Damjanoska et al. Neuroendocrine evidence that (S)-2-(chloro-5-fluoro-indol-l-yl)-1-methylethylamine fumarate (Ro 60-0175) is not a selective 5-hydroxytryptamine2C receptor agonist. J. Pharmacol. Exp. Ther. 2003, 304,1209.
Kennett et al. Effects of Ro 60-0175, a 5-HT2C receptor agonist, in three animal models of anxiety. Eur. J. Pharmacol. 2000, 387, 197.
Martin et al. 5-HT2C receptor agonists: pharmacological characteristics and therapeutic potential. J. Pharmacol. Exp. Ther. 1998, 286, 913.
Certificate of Analysis
Material Safety Data Sheet
CNS
5-HT2C
A17
5-HT2C agonist
Chemical name
(S)-2-(6-Chloro-5-fluoro-indol-1-yl)-1-methyl-ethylamine fumarate
Parent CAS No.
[169675-08-5]
Order
Size
Unit Price
Stock
10 mg
€115.00
In Stock | | axonmedchem |
| Brexpiprazole dihydrochloride - OPC 34712 dihydrochloride | Axon 2335
CAS [913612-38-1]
MF C25H27N3O2S.2HClMW 506.49
Purity:
98%
Soluble in DMSO
Description
Drug candidate in clinical development for psychiatric disorders with high affinity for h5-HT1A (partial agonist), h5-HT2A (antagonist), hD2L (partial agonist), hα1B (antagonist) and hα2C-adrenergic (antagonist) receptors (Ki values <1 nM). Brexpiprazole also shows substantial affinity (Ki <5 nM) for hD3, h5-HT2B, h5-HT7, hα1A and hα1D adrenergic receptors, and moderate affinity for hH1 (Ki =19 nM).
References
Certificates
Categories
Extra info
K. Maeda et al. Brexpiprazole I: in vitro and in vivo characterization of a novel serotonin-dopamine activity modulator. J Pharmacol Exp Ther. 2014 Sep;350(3):589-604.
K. Maeda et al. Brexpiprazole II: antipsychotic-like and procognitive effects of a novel serotonin-dopamine activity modulator. J Pharmacol Exp Ther. 2014 Sep;350(3):605-14.
N. Yoshimi et al. Effects of brexpiprazole, a novel serotonin-dopamine activity modulator, on phencyclidine-induced cognitive deficits in mice: a role for serotonin 5-HT1A receptors. Pharmacol Biochem Behav. 2014 Sep;124:245-9.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
CNS
D2
D3
5-HT1A
5-HT7
5-HT2A
Adrenoceptor α2
Adrenoceptor α1
A17
A19
Drug candidate with high affinity for 5-HT1A, 5-HT2A, D2L, α1B, and α2C-adrenergic receptors
Chemical name
7-(4-(4-(benzo[b]thiophen-4-yl)piperazin-1-yl)butoxy)quinolin-2(1H)-one dihydrochloride
Parent CAS No.
[913611-97-9]
Order
Size
Unit Price
Stock
5 mg
€135.00
In Stock | | axonmedchem |
| Sunepitron hydrochloride - CP 93393 hydrochloride | CP 93393-1 | Axon 1519
CAS [148408-65-5 ]
MF C17H23N5O2.HClMW 365.86
Purity:
99%
Optical purity:
Optically pure
Soluble in water and DMSO
Description
Sunepitron is a selective serotonin 5-HT1A autoreceptor agonist, α2-adrenergic antagonist, and dopamine D2 agonist. Anxiolytic, antidepressant.
References
Certificates
Categories
Extra info
S.T. Colgan et al. Assay and purity evaluation of sunepitron hydrochloride by reversed-phase liquid chromatography using a reference standard composite. J Pharm Biomed Anal. 1998 Nov;18(3):429-40.
J. Silvestre et al. Sunepitron Hydrochloride. Drugs Fut. 1998; 23(2):161-165.
C. Prakash et al. Metabolism and excretion of a novel antianxiety drug candidate, CP-93,393, in Long Evans rats. Differentiation of regioisomeric glucuronides by LC/MS/MS. Drug Metab Dispos. 1997 Nov;25(11):1288-97.
C. Prakash et al. Metabolism and excretion of a new anxiolytic drug candidate, CP-93, 393, in healthy male volunteers. Drug Metab Dispos. 1998 May;26(5):448-56.
Certificate of Analysis
Material Safety Data Sheet
CNS
D2
5-HT1A
Adrenoceptor α2
A17
A19
Pfizer Licensed Products
Anxiolytic and antidepressant drug
Chemical name
1-(((7S,9aS)-2-(pyrimidin-2-yl)octahydro-1H-pyrido[1,2-a]pyrazin-7-yl)methyl)pyrrolidine-2,5-dione hydrochloride
Source information
Pfizer compound; Sold for research purposes under agreement from Pfizer Inc.
Parent CAS No.
[131831-03-3]
Order
Size
Unit Price
Stock
5 mg
€140.00
In Stock | | axonmedchem |
| Fluphenazine decanoate dihydrochloride - Prolixin Decanoate dihydrochloride | Axon 2127
CAS [2376-65-0]
MF C32H44F3N3O2S.2HClMW 664.69
Purity:
99%
Soluble in DMSO
Description
Fluphenazine (available after slow hydrolysis in vivo of the parent molecule) is a potent antipsychotic (Ki values 0.2 nM, 0.11 nM, and 2.0nM for D2, D3, and 5-HT2 receptors, respectively). Fluphenazine exhibits considerable affintiy for 5-HT6 and 5-HT7 receptors (Ki values 15.8nM and 7.9 nM, respectively) as well.
References
Certificates
Categories
Extra info
H.L. Yale et al. Esters of 4-{3-[2-(Trifluoromethyl)phenothiazin-10-yl]propyl}-1-piperazineëthanol as long-acting tranquilizing agents. Synthesis of... J. Med. Chem., 1963, 6, 347-350.
P. Seeman et al. Antipsychotic drugs which elicit little or no parkinsonism bind more loosely than dopamine to brain D2 receptors, yet occupy high levels of these receptors. Mol. Psychiatry. 1998, 3, 123-134.
B.L. Roth et al. Binding of typical and atypical antipsychotic agents to 5-hydroxytryptamine-6 and 5-hydroxytryptamine-7 receptors. J. Pharmacol. Exp. Ther. 1994, 268, 1403-1410.
Certificate of Analysis
Material Safety Data Sheet
CNS
Pain & Inflammation
Endocrinology
D2
D3
A17
Antipsychotic with high affinity for dopamine and serotonin receptors
Chemical name
2-(4-(3-(2-(trifluoromethyl)-10H-phenothiazin-10-yl)propyl)piperazin-1-yl)ethyl decanoate dihydrochloride
Parent CAS No.
[5002-47-1]
Order
Size
Unit Price
Stock
10 mg
€75.00
In Stock | | axonmedchem |
| PNU 22394 hydrochloride | Axon 1247
CAS [15923-42-9]
MF C13H16N2.HClMW 236.74
Purity:
99%
Soluble in DMSO
Description
Potent 5-HT2 ligand (Ki values 18 nM, 18 nM, and 66 nM for 5-HT2A, 5-HT2C, and 5-HT2B, respectively). PNU 22394 is virtually a full agonist at 5-HT2C receptors (87% of 5-HT), but a partial agonist at 5-HT2A (65% of 5-HT), and 5-HT2B (<15% of 5-HT) receptors, and produced a dose-related decrease in food consumption compared to saline-treated control rats.
KEYWORDS: PNU 22394 hydrochloride | supplier | 5-HT2C agonist | PNU22394 | PNU 22394A | CAS [15923-42-9] | [15923-78-1] | Serotonin | 5-HT2C | Agonist | 5-HT2A | 5-HT2B | food | consumption | obesity | weight loss | metabolism | hypophagic | anorexogenic | | axonmedchem |
| Hydroxybuspirone hydrochloride, 6- - BMS 528215 hydrochloride | 6OHB | 6-OH-Bu | Axon 1996
CAS [N.A.]
MF C21H31N5O3.HClMW 437.96
Purity:
98%
Soluble in water and DMSO
Description
A major active metabolite of Buspirone (Axon 1995), a 5-HT1A partial agonist; with improved bioavailability (19%) compared with that for buspirone (1.4%); contributes significantly to the clinical efficacy of buspirone as an anxiolytic agent
References
Certificates
Categories
Extra info
H Wong et al. 6-Hydroxybuspirone is a major active metabolite of buspirone: assessment of pharmacokinetics and 5-hydroxytryptamine1A receptor occupancy in rats. Drug Metab. Dispos. 2007, 35(8), 1387-1392.
RC Dockens et al. Pharmacokinetics of 6-hydroxybuspirone and its enantiomers administered individually or following buspirone administration in humans. Biopharm. Drug Dispos. 2007, 28(7), 393-402.
SJ Nicholson et al. Development of oral extended release formulations of 6-hydroxybuspirone. Biopharm. Drug Dispos. 2012, 33(9), 522-535.
Certificate of Analysis
Material Safety Data Sheet
CNS
5-HT1A
A19
5-HT1A partial agonist
Chemical name
6-hydroxy-8-(4-(4-(pyrimidin-2-yl)piperazin-1-yl)butyl)-8-azaspiro[4.5]decane-7,9-dione hydrochloride
Parent CAS No.
[125481-61-0]
Order
Size
Unit Price
Stock
5 mg
€135.00
In Stock | | axonmedchem |
| Buspirone hydrochloride - Buspar | Axon 1995
CAS [33386-08-2]
MF C21H31N5O2.HClMW 421.96
Purity:
100%
Soluble in water and DMSO
Description
Serotonin 5-HT1A receptor partial agonist; an anxiolytic psychoactive drug used primarily to treat generalized anxiety disorder (GAD); Suggestive evidence that buspirone reverses SSRI-induced sexual dysfunction
References
Certificates
Categories
Extra info
DA Ciraulo et al. Alterations in pharmacodynamics of anxiolytics in abstinent alcoholic men: Subjective responses, abuse liability, and electroencephalographic effects of alprazolam, diazepam, and buspirone. J. Clin. Pharmacol. 1997, 37(1), 64-73.
N Demartinis et al. Prior benzodiazepine use and buspirone response in the treatment of generalized anxiety disorder. J. Clin. Psychiatry 2000, 61(2), 91-94.
Certificate of Analysis
Material Safety Data Sheet
CNS
5-HT1A
A19
5-HT1A partial agonist
Chemical name
8-(4-(4-(pyrimidin-2-yl)piperazin-1-yl)butyl)-8-azaspiro[4.5]decane-7,9-dione hydrochloride
Parent CAS No.
[36505-84-7]
Order
Size
Unit Price
Stock
25 mg
€50.00
In Stock | | axonmedchem |
| Eletriptan hydrobromide - UK 116044-04 | Axon 2050
CAS [177834-92-3]
MF C22H26N2O2S.HBrMW 463.43
Purity:
99%
Optical purity:
Optically pure
Soluble in water and DMSO
Description
Potent and selective 5-HT1B/1D receptor agonist; second generation anti-migraine drug
References
Certificates
Categories
Extra info
P Gupta et al. The in vivo pharmacological profile of eletriptan (UK-116,044): a potent and novel 5-HT(1B/1D) receptor agonist. Eur. J. Pharmacol. 2000, 398(1), 73-81.
PJ Goadsby et al. Eletriptan in acute migraine - A double-blind, placebo-controlled comparison to sumatriptan. Neurology 2000, 54(1), 156.
Certificate of Analysis
Material Safety Data Sheet
Cardiovascular
CNS
5-HT1B
5-HT1D
A19
Pfizer Licensed Products
Selective 5-HT1B/1D receptor agonist
Chemical name
(R)-3-((1-methylpyrrolidin-2-yl)methyl)-5-(2-(phenylsulfonyl)ethyl)-1H-indole hydrobromide
Source information
Pfizer compound; Sold for research purposes under agreement from Pfizer Inc.
Parent CAS No.
[143322-58-1]
Order
Size
Unit Price
Stock
10 mg
€90.00
In Stock | | axonmedchem |
| Blonanserin - AD 5423 | Axon 2353
CAS [132810-10-7]
MF C23H30FN3MW 367.50
Purity:
100%
Soluble in 0.1N HCl(aq) and DMSO
Description
Potent dopamine D2 and serotonin 5-HT2 antagonist (Ki values 0.14 nM and 0.81 nM for human D2L and 5-HT2A receptors respectively) with weak adrenaline-α1 and virtually no dopamine D1 affinity.
References
Certificates
Categories
Extra info
T. Ochi et al. Syntheses and properties of the major hydroxy metabolites in humans of blonanserin AD-5423, a novel antipsychotic agent. Bioorg. Med. Chem. Lett. 2005, 15, 1055-1059.
M. Oka et al. Pharmacological profile of AD-5423, a novel antipsychotic with both potent dopamine-D2 and serotonin-S2 antagonist properties. J. Pharmacol. Exp. Ther. 1993, 264, 158-165.
Certificate of Analysis
Material Safety Data Sheet
CNS
D2
5-HT2
A17
Potent dopamine D2 and serotonin 5-HT2 antagonist
Chemical name
2-(4-ethylpiperazin-1-yl)-4-(4-fluorophenyl)-5,6,7,8,9,10-hexahydrocycloocta[b]pyridine
Parent CAS No.
[132810-10-7]
Order
Size
Unit Price
Stock
10 mg
€65.00
In Stock | | axonmedchem |
| GW 803430 - GW 3430 | Axon 1569
CAS [515141-51-2]
MF C25H24ClN3O3SMW 481.99
Purity:
98%
Soluble in DMSO
Description
Selective, non-peptide antagonist at the melanin concentrating hormone receptor 1 (MCH1 aka MCH R1). In animal studies it has anxiolytic, antidepressant and anorectic effects
References
Certificates
Categories
Extra info
DR Gehlert et al. Preclinical evaluation of melanin-concentrating hormone receptor 1 antagonism for the treatment of obesity and depression. J. Pharmacol. Exp. Ther. 2009, 329 (2), 429–438.
SL Able et al. Localisation of melanin-concentrating hormone receptor 1 in rat brain and evidence that sleep parameters are not altered despite high central receptor occupancy. Eur. J. Pharmacol. 2009, 616(1-3), 101-106.
S Chaki and K Kanuma. Neuropeptide receptors: Novel therapeutic targets for depression and anxiety disorders. Drugs Fut. 2007, 32(9), 809.
Certificate of Analysis
Material Safety Data Sheet
CNS
MCH1
Endocrinology
A5
MCH1 antagonist
Chemical name
6-(4-Chloro-phenyl)-3-[3-methoxy-4-(2-pyrrolidin-1-yl-ethoxy)-phenyl]-3H-thieno[3,2-d]pyrimidin-4-one
Parent CAS No.
[515141-51-2]
Order
Size
Unit Price
Stock
5 mg
€85.00
In Stock | | axonmedchem |
| Risperidone - R 64766 | Axon 1454
CAS [106266-06-2]
MF C23H27FN4O2MW 410.48
Purity:
99%
Soluble in DMSO
Description
5-HT2 and dopamine D2 antagonist with high affinity for 5-HT7 receptors; an atypical antipsychotic in the treatment of psychotic disorders with negative and positive symptomatology
References
Certificates
Categories
Extra info
Leysen et al. Biochemical profile of risperidone, a new antipsychotic. J. Pharmacol. Exp. Ther. 1988, 247, 661.
Stathis et al. Risperidone: a novel antipsychotic with many "atypical" properties. Psychopharmacol. 1996, 127, 181.
A Szarfman et al. Atypical antipsychotics and pituitary tumors: a pharmacovigilance study. Pharmacotherapy 2006, 26(6), 748–58.
Certificate of Analysis
Material Safety Data Sheet
CNS
D2
5-HT7
5-HT2
A17
Atypical antipsychotic
Chemical name
3-{2-[4-(6-Fluoro-benzo[d]isoxazol-3-yl)-piperidin-1-yl]-ethyl}-2-methyl-6,7,8,9-tetrahydro-pyrido[1,2-a]pyrimidin-4-one
Parent CAS No.
[106266-06-2]
Order
Size
Unit Price
Stock
10 mg
€75.00
In Stock | | axonmedchem |
| Asenapine maleate - ORG 5222 | Axon 1503
CAS [85650-56-2]
MF C17H16ClNO.C4H4O4MW 401.84
Purity:
99%
Soluble in DMSO
Description
An atypical antipsychotic for the treatment of schizophrenia and acute mania associated with bipolar disorder; Displays high affinity antagonistic activities at many receptors, including dopamine (D) and serotonin (5-HT) receptor subtypes. However, it has much lower affinity (pKi < 5) for the muscarinic acetylcholine receptors
References
Certificates
Categories
Extra info
M Shahid et al. Asenapine: a novel psychopharmacologic agent with a unique human receptor signature. J. Psychopharmacol. 2009, 23(1), 65–73.
Certificate of Analysis
Material Safety Data Sheet
CNS
D2
D3
5-HT1A
5-HT1B
5-HT1D
5-HT7
5-HT2A
5-HT2C
5-HT2
Adrenoceptor α2
H2
D4
Adrenoceptor α1
H1
A17
Atypical antipsychotic
Chemical name
(3aS,12bS)-5-Chloro-2,3,3a,12b-tetrahydro-2-methyl-1H-dibenz[2,3:6,7]oxepino[4,5-c]pyrrole maleate
Parent CAS No.
[65576-45-6]
Order
Size
Unit Price
Stock
10 mg
€75.00
In Stock | | axonmedchem |
| Ziprasidone hydrochloride - CP 88059 | Axon 1446
CAS [122883-93-6]
MF C21H21ClN4OS.HClMW 449.40
Purity:
99%
Soluble in DMSO
Description
A 5-HT2A/5-HT2C and dopamine D2 antagonist, 5-HT1A agonist; an atypical antipsychotic for the treatment of schizophrenia and acute bipolar disorder including manic and mixed episodes; Oral bioavailability 59%; Antipsychotic effects at oral doses of 20 mg.
KEYWORDS: Ziprasidone HCl | supplier | Atypical antipsychotic | CP 88059 | CP88059 | CP-88059 | CAS [122883-93-6] | [146939-27-7] | Serotonin; Dopamine | 5-HT | Antagonist | Agonist | GPCR | schizophrenia | bipolar | disorder | manic episodes | oral | | axonmedchem |
| Amisulpride - DAN 2163 | Axon 1381
CAS [71675-85-9]
MF C17H27N3O4SMW 369.48
Purity:
99%
Soluble in 0.1N HCl(aq)
Description
Dopamine D2 and D3 receptor antagonist (Ki 2.8 and 3.2 nM for D2 and D3 respectively); Claimed to be atypical antipsychotic with low incidence of EPS
References
Certificates
Categories
Extra info
H Loo et al. Amisulpride versus placebo in the medium-term treatment of the negative symptoms of schizophrenia. Br. J. Psychiatry 1999, 170, 18-22.
H Choemaker et al. Neurochemical characteristics of amisulpride, an atypical dopamine D2/D3 receptor antagonist with both presynaptic and limbic selectivity. J. Pharmacol. Exp. Ther. 1997, 280(1), 83-97.
Certificate of Analysis
Material Safety Data Sheet
CNS
D2
D3
A17
D2 and D3 antagonist
Chemical name
4-Amino-5-ethanesulfonyl-N-(1-ethyl-pyrrolidin-2-ylmethyl)-2-methoxy-benzamide
Parent CAS No.
[71675-85-9]
Order
Size
Unit Price
Stock
10 mg
€45.00
In Stock | | axonmedchem |
| Iloperidone | Axon 1493
CAS [133454-47-4]
MF C24H27FN2O4MW 426.48
Purity:
99%
Soluble in DMSO
Description
An atypical antipsychotic for the treatment of schizophrenia, acting upon and antagonizing specific neurotransmitters, particularly multiple dopamine and serotonin receptor subtypes
References
Certificates
Categories
Extra info
MP Szewczak et al. The pharmacological profile of iloperidone, a novel atypical antipsychotic agent. J Pharmacol. Exp. Ther. 1995, 274(3). 1404–13.
L Scott. Iloperidone: In Schizophrenia. CNSDrugs 2009, 23(10), 867-880.
Certificate of Analysis
Material Safety Data Sheet
CNS
D2
D3
5-HT1D
5-HT2A
5-HT2C
Adrenoceptor α2
D4
Adrenoceptor α1
H1
A17
Atypical antipsychotic
Chemical name
1-(4-{3-[4-(6-Fluoro-benzo[d]isoxazol-3-yl)-piperidin-1-yl]-propoxy}-3-methoxy-phenyl)-ethanone
Parent CAS No.
[133454-47-4]
Order
Size
Unit Price
Stock
10 mg
€85.00
In Stock | | axonmedchem |
| Quetiapine fumarate - ICI 204636 | ZD 5077 | ZM 204636 | Axon 1354
CAS [111974-72-2]
MF C21H25N3O2S.½C4H4O4MW 441.54
Purity:
99%
Soluble in DMSO
Description
Atypical antipsychotic; Quetiapine is a moderate 5-HT2, weak dopamine D2 and α2 receptor antagonist
References
Certificates
Categories
Extra info
H. Wetzel et al. Seroquel (ICI 204 636), a putative "atypical" antipsychotic, in schizophrenia with positive symptomatology: results of an open clinical trial and changes of neuroendocrinological and EEG parameters. Psychopharm. 1995, 119, 231-238.
C Vesely et al. Remission of severe tardive dyskinesia in a shizophrenic patient treated with atypical antipsychotic substance quetiapine. Int. Clin. Psychopharmacol. 2000, 15, 57-60.
Certificate of Analysis
Material Safety Data Sheet
CNS
D2
D3
5-HT2
Adrenoceptor α2
Adrenoceptor α1
H1
A17
Atypical antipsychotic
Chemical name
2-[2-(4-Dibenzo[b,f][1,4]thiazepin-11-yl-piperazin-1-yl)-ethoxy]-ethanol (E)-But-2-enedioate
Parent CAS No.
[111974-69-7]
Order
Size
Unit Price
Stock
10 mg
€75.00
In Stock | | axonmedchem |
| SKF 83566 hydrobromide | Axon 1236
CAS [108179-91-5]
MF C17H18BrNO.HBrMW 413.15
Purity:
99%
Soluble in water and DMSO
Description
Selective dopamine D1-like receptor antagonist
References
Certificates
Categories
Extra info
R Pedrosa et al. Defective D1-like receptor-mediated inhibition of the Cl–/HCO3– exchanger in immortalized SHR proximal tubular epithelial cells. Am. J. Physiol. Renal. Physiol. 2004, 286, F1120-F1126.
Meyeret al. Effects of dopamine D1 antagonists SCH23390 and SK&F83566 on locomotor activities in rats. Pharmacol. Biochem. Behav. 1993, 44, 429.
Certificate of Analysis
Material Safety Data Sheet
CNS
DRI
D1
A17
D1 antagonist
Chemical name
8-Bromo-3-methyl-5-phenyl-2,3,4,5-tetrahydro-1H-benzo[d]azepin-7-ol hydrobromide
Parent CAS No.
[99295-33-7]
Order
Size
Unit Price
Stock
10 mg
€70.00
In Stock | | axonmedchem |
| GMC 1-165 | Axon 1152
CAS [156632-07-4]
MF C18H20N4OMW 308.38
Purity:
99%
Soluble in 0.1N HCl(aq) and DMSO
Description
Analogue of clozapine (Axon 1146); devoid of DA affinities but with affinities at 5-HT2A/2C and hM1 receptors.
Another analogue and metabolite of cloazapine, with 8-hydroxy moiety, GMC1-116 ( | | axonmedchem |
| GMC 1-116 | Axon 1151
CAS [63687-94-5]
MF C18H20N4OMW 308.38
Purity:
99%
Soluble in 0.1N HCl(aq) and DMSO
Description
Analogue and metabolite of clozapine (Axon 1146); devoid of DA and α1 affinities, with weak 5-HT2 affinities but high M1 affinity (IC50=27 nM).
Another analogue and metabolite of cloazapine, with 2-Hydroxy moiety, | | axonmedchem |
| GMC 2-83 | Axon 1150
CAS [183140-98-9]
MF C19H18F3N3O4SMW 441.42
Purity:
99%
Soluble in 0.1N HCl(aq) and DMSO
Description
Atypical antipsychotic lack of muscarinic activity
References
Certificates
Categories
Extra info
Liao, Y. et al. Synthesis and pharmacological evaluation of triflate-substituted analogues of Clozapine: Identification of a novel atypical neuroleptic. J. Med. Chem. 1997, 40, 4146-4153.
Y. Liao et al. New sulfonyloxy piperazinyldibenzazapines as potential atypical antipsychotics: chemistry and pharmacological evaluation. J. Med. Chem. 1999,42, 2235-2244.
Jackson, D; Wikström, H; Liao, Y. Is clozapine an (partial) agonist at both dopamine D1 and D2 receptors? Psychopharm. 1998, 138, 213-214.
Certificate of Analysis
Material Safety Data Sheet
CNS
D2
5-HT2A
Adrenoceptor α1
A17
Atypical antipsychotic
Chemical name
11-(4-Methylpiperazin-1-yl)dibenzo[b,f][1,4]oxazepin-2-yl trifluoromethanesulfonate
Parent CAS No.
[183140-98-9]
Order
Size
Unit Price
Stock
10 mg
€145.00
In Stock | | axonmedchem |
| GMC 61-39 | Axon 1149
CAS [234113-94-1]
MF C19H18ClF3N4O3SMW 474.88
Purity:
98%
No solubility data
Description
Clozapine-like atypical antipsychotic
References
Certificates
Categories
Extra info
Liao, Y. et al. Synthesis and pharmacological evaluation of triflate-substituted analogues of Clozapine: Identification of a novel atypical neuroleptic. J. Med. Chem. 1997, 40, 4146-4153.
Y. Liao et al. New sulfonyloxy piperazinyldibenzazapines as potential atypical antipsychotics: chemistry and pharmacological evaluation. J. Med. Chem. 1999,42, 2235-2244.
Jackson, D; Wikström, H; Liao, Y. Is clozapine an (partial) agonist at both dopamine D1 and D2 receptors? Psychopharm. 1998, 138, 213-214.
CNS
D2
5-HT2A
Adrenoceptor α1
A17
Atypical antipsychotic
Chemical name
Trifluoro-methanesulfonic acid 8-chloro-11-(4-methyl-piperazin-1-yl)-5H-dibenzo[b,e][1,4]diazepin-2-yl ester
Parent CAS No.
[234113-94-1]
Inquire | | axonmedchem |
| GMC 1-169 | Axon 1148
CAS [183140-97-8]
MF C19H19F3N4O3SMW 440.44
Purity:
99%
Soluble in DMSO
Description
Atypical antipsychotic lack of muscarinic activity
References
Certificates
Categories
Extra info
Liao, Y. et al. Synthesis and pharmacological evaluation of triflate-substituted analogues of Clozapine: Identification of a novel atypical neuroleptic. J. Med. Chem. 1997, 40, 4146-4153.
Y. Liao et al. New sulfonyloxy piperazinyldibenzazapines as potential atypical antipsychotics: chemistry and pharmacological evaluation. J. Med. Chem. 1999,42, 2235-2244.
Jackson, D; Wikström, H; Liao, Y. Is clozapine an (partial) agonist at both dopamine D1 and D2 receptors? Psychopharm. 1998, 138, 213-214.
Certificate of Analysis
Material Safety Data Sheet
CNS
D2
5-HT2A
Adrenoceptor α1
A17
Atypical antipsychotic
Chemical name
11-(4-Methylpiperazin-1-yl)-5H-dibenzo[b,e][1,4]diazepin-2-yl trifluoromethanesulfonate
Parent CAS No.
[183140-97-8]
Order
Size
Unit Price
Stock
10 mg
€145.00
In Stock | | axonmedchem |
| Isoclozapine | Axon 1147
CAS [1977-08-8]
MF C18H19ClN4MW 326.82
Purity:
98%
Soluble in DMSO
Description
Typical antipsychotic; 2-Cl analogue of clozapine, atypical antipsychotic. Useful tool compound in comparison with clozapine; distinctly typical vs atypical profile
References
Certificates
Categories
Extra info
Kapur et al. Increasing D2 affinity results in the loss of clozapine's atypical antipsychotic action. Neuroreport. 2002, 13, 831-835.
Seeman P. Atypical Antipsychotics: Mechanisms of Action. Can. J. Psychiatry. 2002, 47, 27-38.
Certificate of Analysis
Material Safety Data Sheet
CNS
D2
D3
5-HT2A
5-HT2C
D4
D1
A17
Typical antipsychotic
Chemical name
2-Chloro-11-(4-methyl-piperazin-1-yl)-5H-dibenzo[b,e][1,4]diazepine
Parent CAS No.
[1977-08-8]
Order
Size
Unit Price
Stock
10 mg
€135.00
In Stock | | axonmedchem |
| Clozapine | Axon 1146
CAS [5786-21-0]
MF C18H19ClN4MW 326.82
Purity:
99%
Soluble in DMSO
Description
A putative atypical antipsychotic; Clozapine has been shown to be superior in efficacy in treating schizophrenia, however, the drug is not indicated for first-line use because of its association with agranulocytosis and seizures
References
Certificates
Categories
Extra info
Kapur et al. Increasing D2 affinity results in the loss of clozapine's atypical antipsychotic action. Neuroreport. 2002, 13, 831-835.
Seeman P. Atypical Antipsychotics: Mechanisms of Action. Can. J. Psychiatry. 2002, 47, 27-38.
Certificate of Analysis
Material Safety Data Sheet
CNS
5-HT6
5-HT7
5-HT2A
5-HT2C
5-HT2
Adrenoceptor α2
H2
D4
H4
CHRM3
Adrenoceptor α1
H1
CHRM4
CHRM1
CHRM5
A17
Atypical antipsychotic
Chemical name
8-Chloro-11-(4-methyl-piperazin-1-yl)-5H-dibenzo[b,e][1,4]diazepine
Parent CAS No.
[5786-21-0]
Order
Size
Unit Price
Stock
10 mg
€45.00
In Stock | | axonmedchem |
| Aripiprazole, thio- | Axon 1144
CAS [573691-04-0]
MF C23H27Cl2N3OSMW 464.45
Purity:
98%
No solubility data
Description
Atypical antipsychotic
References
Certificates
Categories
Extra info
Zhang et al. Recent advances towards the discovery of dopamine receptor ligands. Expert Opinion on Ther. Patent. 2006, 16(5), 587-630.
Wikstrom, Dijkstra and Liao. Thio-carbostyril derivative, its N-oxides and the N-oxides of arippiprazole. WO/2003/064393
CNS
D2
D3
5-HT1A
5-HT7
5-HT2A
5-HT2
D1
A17
Atypical antipsychotic
Chemical name
7-{4-[4-(2,3-Dichloro-phenyl)-piperazin-1-yl]-butoxy}-3,4-dihydro-1H-quinoline-2-thione
Parent CAS No.
[573691-04-0]
Inquire | | axonmedchem |
| Aripiprazole - OPC 14597 | OPC 31 | Axon 1143
CAS [129722-12-9]
MF C23H27Cl2N3O2MW 448.39
Purity:
99%
Soluble in DMSO
Description
Partial dopamine D2 and 5-HT1A receptor agonist and 5-HT2A receptor antagonist; T1/2 about 46 hrs; oral active; atypical antipsychotic
References
Certificates
Categories
Extra info
C.P. Lawler et al. Interactions of the novel antipsychotic aripiprazole (OPC-14597) with dopamine and serotonin receptor subtypes. Neuropsychopharmacology. 1999, 20, 612-627.
Certificate of Analysis
Material Safety Data Sheet
CNS
D2
D3
5-HT1A
5-HT7
5-HT2A
5-HT2
D1
A17
Atypical antipsychotic
Chemical name
7-{4-[4-(2,3-Dichloro-phenyl)-piperazin-1-yl]-butoxy}-3,4-dihydro-1H-quinolin-2-one
Parent CAS No.
[129722-12-9]
Order
Size
Unit Price
Stock
10 mg
€75.00
In Stock | | axonmedchem |
| Sertindole - LU 23-174 | Axon 1141
CAS [106516-24-9]
MF C24H26ClFN4OMW 440.94
Purity:
99%
Soluble in DMSO
Description
5-HT2, D2 and α1 antagonist; Sertindole is an atypical antipsychotic with prominent selectivity for the brain limbic area and long lasting
References
Certificates
Categories
Extra info
A Hale, JM Azorin, S Kasper et al. Sertindole is associated with a low level of extrapyramidal symptoms in schizophrenic patients: Results of a phase III trial. Int. J. Psychiatry Clin. Pract. 2000, 4, 47-54.
S Miyamoto et al. Treatments for schizophrenia: a critical review of pharmacology and mechanisms of action of antipsychotic drugs. Mol. Psychiatry2005, 10, 79-104.
Certificate of Analysis
Material Safety Data Sheet
CNS
D2
5-HT2
A17
5-HT2, D2 and α1 adrenoceptor antagonist
Chemical name
1-(2-{4-[5-Chloro-1-(4-fluoro-phenyl)-1H-indol-3-yl]-piperidin-1-yl}-ethyl)-imidazolidin-2-one
Parent CAS No.
[106516-24-9]
Order
Size
Unit Price
Stock
10 mg
€82.00
In Stock | | axonmedchem |
| VU 6008667 | Axon 2739
CAS [2092923-21-0]
MF C24H17ClF2N2O2MW 438.85
Purity:
99%
Optical purity:
98% e.e.
Soluble in DMSO and Ethanol
Description
VU6008667 is a selective negative allosteric modulator (NAM) of M5 muscarinic acetylcholine receptor (mAChR) with IC50 values of 1.2 and 1.6 μM in human and rat M5, respectively. Moreover, VU6008667 has high CNS penetration and shows a desired short half-life in rat (t1/2 = 2.3 h) useful for addiction studies.
KEYWORDS: VU 6008667 | supplier | M5 NAM | VU6008667 | VU-6008667 | CAS [2092923-21-0] | Acetylcholine | CHRM5 | NAM | Receptors | Addiction | Muscarinic | | axonmedchem |
| WAY 100635 trihydrochloride, desmethyl- - DWAY | Axon 1087
CAS [146715-34-6]
MF C24H32N4O2.3HClMW 517.92
Purity:
98%
Soluble in water and DMSO
Description
Precursor for labeling the 5-HT1A antagonist, WAY 100635; PET radioligand
References
Certificates
Categories
Extra info
B Andrée et al. The PET Radioligand [carbonyl-11C]Desmethyl-WAY-100635 Binds to 5-HT1A Receptors and Provides a Higher Radioactive Signal Than [carbonyl-11C]WAY-100635 in the Human Brain. J. Nuclear Medicine 2002, 43(3), 292-303.
Certificate of Analysis
Material Safety Data Sheet
CNS
5-HT1A
5-HT2
D4
Adrenoceptor α1
A17
Building Block for labelled 5-HT1A antagonist
Chemical name
Cyclohexanecarboxylic acid {2-[4-(2-hydroxy-phenyl)-piperazin-1-yl]-ethyl}-pyridin-2-yl-amide trihydrochloride
Parent CAS No.
[146715-07-3]
Order
Size
Unit Price
Stock
10 mg
€145.00
In Stock | | axonmedchem |
| WAY 100635 hydrochloride | Axon 1086
CAS [146714-97-8]
MF C25H34N4O2.xHClMW 459.02
Purity:
99%
Soluble in water and DMSO
Description
Prototypical 5-HT1A receptor antagonist with D4 agonist activity (Ki values 2.2 nM, 6260 nM, 24 nM, >10,000 nM, 20 nM, 322 nM, and 16 nM for 5-HT1A, 5-HT2A, 5-HT2B, 5-HT7, α1A, α1B, and D4, respectively).
The maleate salt of WAY 100635 is available as well (Axon 2424).
Prime Source Information | | axonmedchem |
| INK 128 | Axon 2142
CAS [1224844-38-5]
MF C15H15N7OMW 309.33
Purity:
99%
Soluble in 0.1N HCl(aq) and DMSO
Description
Potent and selective mTOR inhibitor.
KEYWORDS: INK 128 | supplier | mTOR inhibitor | MLN 0128 | Sapanisertib | INK128 | MLN0128 | CAS [1224844-38-5] | Phosphatidylinositol | mTOR | Inhibitor | | axonmedchem |
| Rapamycin - Sirolimus | Axon 2069
CAS [53123-88-9]
MF C51H79NO13MW 914.17
Purity:
98%
Soluble in DMSO
Description
Specific inhibitor of mTOR (mammalian target of Rapamycin); it binds the cytosolic protein FKBP12 and inhibits mTOR pathway by directly binding the mTORC1. Rapamycin selectively inhibits interleukin-2 (IL-2) activation of p70 S6 kinase. It prevents activation of T cells and B cells by inhibiting their response to IL-2. An immunosuppressant drug used to prevent rejection in organ transplantation, especially useful in kidney transplants; also used as a coronary stent coating
References
Certificates
Categories
Extra info
CJ Kuo et al. Rapamycin selectively inhibits interleukin-2 activation of p70 S6 kinase. Nature 1992, 358(6381), 70-73.
EJ Brown et al. A mammalian protein targeted by G1-arresting rapamycin-receptor complex. Nature 1994, 369(6483) 756-758.
S Kobayashi et al. Rapamycin, a specific inhibitor of the mammalian target of rapamycin, suppresses lymphangiogenesis and lymphatic metastasis. Cancer Sci. 2007, 98(5), 726-33.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Immunology
Immunomodulator
mTOR
PI3K-Akt-mTOR
EC 2.7.11.1
Pfizer Licensed Products
Specific inhibitor of mTOR; binds to FKBP12
Chemical name
(3S,6R,7E,9R,10R,12R,14S,15E,17E,19E,21S,23S,26R,27R,34aS)-9,10,12,13,14,21,22,23,24,25,26,27,32,33,34,34a-Hexadecahydro-9,27-dihydroxy-3-[(1R)-2-[(1S,3R,4R)-4-hydroxy-3-methoxycyclohexyl]-1-methylethyl]-10,21-dimethoxy-6,8,12,14,20,26-hexamethyl-23,27-ep
Source information
Pfizer compound; Sold for research purposes under agreement from Pfizer Inc.
Parent CAS No.
[53123-88-9]
Order
Size
Unit Price
Stock
2 mg
€85.00
In Stock | | axonmedchem |
| NVP-BGT226 - BGT 226 | Axon 2029
CAS [1245537-68-1]
MF C28H25F3N6O2.C4H4O4MW 650.60
Purity:
99%
Soluble in DMSO
Description
Orally active dual PI3K/mTOR inhibitor; induces cell cycle arrest and regulates survivin gene expression in human pancreatic cancer cell lines; inhibits growth in common myeloma cell lines and primary myeloma cells at nanomolar concentrations in a time-dependent and dose-dependent manner
References
Certificates
Categories
Extra info
KY Chang et al. Novel phosphoinositide 3-kinase/mTOR dual inhibitor, NVP-BGT226, displays potent growth-inhibitory activity against human head and neck cancer cells in vitro and in vivo. Clin. Cancer Res. 2011, 17(22), 7116-26.
W Glienke et al. The dual PI3K/mTOR inhibitor NVP-BGT226 induces cell cycle arrest and regulates Survivin gene expression in human pancreatic cancer cell lines. Tumour Biol. 2012, 33(3), 757-765.
P Baumann et al. Simultaneous targeting of PI3K and mTOR with NVP-BGT226 is highly effective in multiple myeloma. Anticancer Drugs. 2012, 23(1), 131-138.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Cycle Regulation
Cell Signaling & Oncology
PI3K
mTOR
PI3K-Akt-mTOR
EC 2.7.11.1
Orally active dual PI3K/mTOR inhibitor
Chemical name
8-(6-methoxypyridin-3-yl)-3-methyl-1-(4-(piperazin-1-yl)-3-(trifluoromethyl)phenyl)-1H-imidazo[4,5-c]quinolin-2(3H)-one maleate
Parent CAS No.
[915020-55-2]
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5 mg
€120.00
In Stock | | axonmedchem |
| PF 04691502 | Axon 1855
CAS [1013101-36-4]
MF C22H27N5O4MW 425.48
Purity:
99%
Soluble in DMSO
Description
Potent, selective, oral and ATP-competitive inhibitor of class I PI3K (Ki: 1-2 nM) and mTOR kinases (Ki: 16 nM); it inhibits PI3K/mTOR signaling and induces cell cycle arrest in cancer cells
References
Certificates
Categories
Extra info
J Yuan et al. PF-04691502, a potent and selective oral inhibitor of PI3K and mTOR kinases with antitumor activity. Mol. Cancer Ther. 2011, 10, 2189.
H Cheng et al. Discovery of the highly potent PI3K/mTOR dual inhibitor PF-04691502 through structure based drug design. Med. Chem. Commun. 2010, 1, 139-144.
Certificate of Analysis
Material Safety Data Sheet
Cell Cycle Regulation
Cell Signaling & Oncology
PI3K
mTOR
PI3K-Akt-mTOR
EC 2.7.11.1
Pfizer Licensed Products
PI3K and mTOR tyrosine kinase inhibitor
Chemical name
2-amino-8-((1r,4r)-4-(2-hydroxyethoxy)cyclohexyl)-6-(6-methoxypyridin-3-yl)-4-methylpyrido[2,3-d]pyrimidin-7(8H)-one
Source information
Pfizer compound; Sold for research purposes under agreement from Pfizer Inc.
Parent CAS No.
[1013101-36-4]
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Size
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Stock
5 mg
€90.00
In Stock | | axonmedchem |
| Torin 2 | Axon 1834
CAS [1223001-51-1]
MF C24H15F3N4OMW 432.40
Purity:
99%
Soluble in DMSO
Description
Potent, selective, orally available and ATP-competitive mTOR inhibitor (IC50: 2.1 nM for mTORC1), which possesses an EC50 of 0.25 nM for inhibiting cellular mTOR activity and exhibited 800-fold selectivity over PI3K (EC50: 200 nM) and over 100-fold binding selectivity relative to 440 other protein kinases
References
Certificates
Categories
Extra info
Q Liu et al. Discovery of 9-(6-aminopyridin-3-yl)-1-(3-(trifluoromethyl)phenyl)benzo[h][1,6]naphthyridin-2(1H)-one (Torin2) as a potent, selective, and orally available (mTOR) inhibitor for treatment of cancer. J. Med. Chem. 2011, 54(5), 1473-1480.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
mTOR
PI3K-Akt-mTOR
EC 2.7.11.1
mTOR inhibitor
Chemical name
9-(6-aminopyridin-3-yl)-1-(3-(trifluoromethyl)phenyl)benzo[h][1,6]naphthyridin-2(1H)-one
Parent CAS No.
[1223001-51-1]
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5 mg
€105.00
In Stock | | axonmedchem |
| Torin 1 | Axon 1833
CAS [1222998-36-8]
MF C35H28F3N5O2MW 607.62
Purity:
98%
Poorly soluble in DMSO
Description
Highly potent, selective and ATP-competitive mTOR inhibitor, with IC50 to be 2 and 10 nM for mTORC1 and mTORC2 respectively; Torin1 exhibits 1000-fold selectivity for mTOR over PI3K (EC50 = 1800 nM) and exhibits 100-fold binding selectivity relative to 450 other protein kinases
References
Certificates
Categories
Extra info
Q Liu et al. Discovery of 1-(4-(4-Propionylpiperazin-1-yl)-3-(trifluoromethyl)phenyl)-9-(quinolin-3-yl)benzo[h][1,6]naphthyridin-2(1H)-one as a Highly Potent, Selective mTOR Inhibitor for the Treatment of Cancer. J. Med. Chem. 2010, 53(19), 7146–7155.
Q Liu et al. Discovery of 9-(6-aminopyridin-3-yl)-1-(3-(trifluoromethyl)phenyl)benzo[h][1,6]naphthyridin-2(1H)-one (Torin2) as a potent, selective, and orally available (mTOR) inhibitor for treatment of cancer. J. Med. Chem. 2011, 54(5), 1473-1480.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
mTOR
PI3K-Akt-mTOR
EC 2.7.11.1
mTOR inhibitor
Chemical name
1-(4-(4-propionylpiperazin-1-yl)-3-(trifluoromethyl)phenyl)-9-(quinolin-3-yl)benzo[h][1,6]naphthyridin-2(1H)-one
Parent CAS No.
[1222998-36-8]
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5 mg
€105.00
In Stock | | axonmedchem |
| PKI 587 - PF 05212384 | Axon 1807
CAS [1197160-78-3]
MF C32H41N9O4MW 615.73
Purity:
99%
Moderately soluble in DMSO
Description
Highly potent PI3K/mTOR kinase inhibitor; PKI-587 inhibits PI3K-α, β, γ, δ isoforms and mTOR with IC50 of 0.4, 6.0, 5.4, 6.0 and 1.6 nM respectively. PKI-587 inhibits mTOR TOC1 kinase activity in human MDA-MB-361 cells assessed as surppression of 4EBP1 phosphorylation at <30 nM; PKI-587 inhibits Akt S473 phosphorylation in human MDA-MB-361 cells and Akt T308 phosphorylation in human MDA-MB-361 cells with IC50 of 8nM and 10 nM
References
Certificates
Categories
Extra info
R Mallon et al. Antitumor efficacy of PKI-587, a highly potent dual PI3K/mTOR kinase inhibitor. Clin Cancer Res. 2011, 17(10), 3193-203.
R Gedaly et al. PKI-587 and Sorafenib Targeting PI3K/AKT/mTOR and Ras/Raf/MAPK Pathways Synergistically Inhibit HCC Cell Proliferation. J. Surg. Res. 2011, 1-7.
AM Venkatesan et al. Bis(morpholino-1,3,5-triazine) derivatives: Potent adenosine 5’-triphosphate competitive phosphatidylinositol-3-kinase/mammalian target of rapamycin inhibitors: Discovery of compound 26 (PKI-587) (...). J. Med. Chem. 2010, 53, 2636.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
PI3K
mTOR
PI3K-Akt-mTOR
EC 2.7.11.1
Pfizer Licensed Products
Dual PI3K and mTOR inhibitor
Chemical name
1-(4-(4-(dimethylamino)piperidine-1-carbonyl)phenyl)-3-(4-(4,6-dimorpholino-1,3,5-triazin-2-yl)phenyl)urea
Source information
Pfizer compound; Sold for research purposes under agreement from Pfizer Inc.
Parent CAS No.
[1197160-78-3]
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Size
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Stock
5 mg
€90.00
In Stock | | axonmedchem |