| 产品标题 |
产品货号 |
产品规格 |
厂家 |
| S 14506, desmethyl- | Axon 1089
CAS [135722-26-8]
MF C23H24FN3O2MW 393.45
Purity:
98%
No solubility data
Description
Precursor for labeling the 5-HT1A agonist, S14506, for PET study
References
Certificates
Categories
Extra info
LU et al. Alternative methods for labeling the 5-HT[1A] receptor agonist, 1-[2-(4-fluorobenzoylamino)ethyl]-4-(7-methoxynaphthyl)piperazine (S14506), with carbon-11 or fluorine-18. J. Labelled Compd. Radiopharm. 2005, 48(13), 971-981.
Certificate of Analysis
Material Safety Data Sheet
CNS
5-HT1A
5-HT1B
5-HT2
A19
Building Block for labelled 5-HT1A agonist
Chemical name
4-Fluoro-N-{2-[4-(7-hydroxy-naphthalen-1-yl)-piperazin-1-yl]-ethyl}-benzamide
Parent CAS No.
[135722-26-8]
Inquire | | axonmedchem |
| Hydroxy-DPAT hydrobromide, (R)-(+)-8- | Axon 1016
CAS [78095-19-9]
MF C16H25NO.HBrMW 328.29
Purity:
98%
Optical purity:
98% ee
Soluble in DMSO
Description
Full 5-HT1A receptor agonist, more active enantiomer of (±)-8-hydroxy-DPAT (Axon 1015)
References
Certificates
Categories
Extra info
T Yoshitake and J Kehr. Differential effects of (R)-, (R, S)- and (S)-8-hydroxy-2-(di-n-propylamino)tetralin on hippocampal serotonin release and induction of hypothermia in awake rats. Life Sci. 2004, 74, 2865.
LJ Cornfield et al. Intrinsic activity of enantiomers of 8-hydroxy-2-(di-n-propylamino)tetralin and its analogs at 5-hydroxytryptamine1A receptors that are negatively coupled to adenylate cyclase. Mol. Pharmacol. 1991, 39, 780.
Certificate of Analysis
Material Safety Data Sheet
CNS
5-HT1A
A19
5-HT1A agonist
Chemical name
(R)-7-Dipropylamino-5,6,7,8-tetrahydro-naphthalen-1-ol hydrobromide
Parent CAS No.
[80300-09-0]
Order
Size
Unit Price
Stock
10 mg
€105.00
In Stock | | axonmedchem |
| S 14506 | Axon 1088
CAS [135722-25-7]
MF C24H26FN3O2MW 407.48
Purity:
98%
Soluble in DMSO and Ethanol
Description
Very potent and selective 5-HT1A agonist
References
Certificates
Categories
Extra info
G Milligan et al. S 14506: novel receptor coupling at 5-HT1A receptors. Neuropharmacology. 2001, 40, 334.
AJ Goudie. Assessment of the dependence potential of the potent high-efficacy 5-HT1A agonist S-14506 in rats. J Psychopharmacol. 1994, 8(4), 213-221.
FC Colpaert et al. S 14506: A novel, potent, high-efficacy 5-HT1A agonist and potential anxiolytic agent. Drug Develop. Res. 1992, 26(1), 21–48.
Certificate of Analysis
Material Safety Data Sheet
CNS
5-HT1A
5-HT1B
5-HT2
A19
5-HT1A agonist
Chemical name
4-Fluoro-N-{2-[4-(7-methoxy-naphthalen-1-yl)-piperazin-1-yl]-ethyl}-benzamide
Parent CAS No.
[135722-25-7]
Order
Size
Unit Price
Stock
5 mg
€85.00
In Stock | | axonmedchem |
| BQR695 - NVP-BQR695 | Axon 2801
CAS [1513879-21-4]
MF C19H20N4O3MW 352.39
Purity:
99%
Soluble in DMSO
Description
BQR695 is a PI4K inhibitor which displays potency against both human PI4KIIIβ and Plasmodium falciparum asexual blood stages (IC50 values of 90 nM and 71 nM, respectively). Antimalarial compound.
KEYWORDS: BQR695 | supplier | PI4K inhibitor | NVP-BQR695 | BQR 695 | BQR-695' | CAS [1513879-21-4] | Phosphatidylinositol | PI4K | Inhibitor | Enzymes | PI4KIIIβ | Malaria | | axonmedchem |
| Hydroxy-DPAT hydrobromide, 8- - DPAT, 8-OH- | Axon 1015
CAS [76135-31-4]
MF C16H25NO.HBrMW 328.29
Purity:
98%
Soluble in DMSO
Description
Standard selective 5-HT1A receptor agonist
References
Certificates
Categories
Extra info
T Yoshitake and J Kehr. Differential effects of (R)-, (R, S)- and (S)-8-hydroxy-2-(di-n-propylamino)tetralin on hippocampal serotonin release and induction of hypothermia in awake rats. Life Sci. 2004, 74, 2865.
LJ Cornfield et al. Intrinsic activity of enantiomers of 8-hydroxy-2-(di-n-propylamino)tetralin and its analogs at 5-hydroxytryptamine1A receptors that are negatively coupled to adenylate cyclase. Mol. Pharmacol. 1991, 39, 780.
Certificate of Analysis
Material Safety Data Sheet
CNS
5-HT1A
A19
5-HT1A agonist
Chemical name
7-Dipropylamino-5,6,7,8-tetrahydro-naphthalen-1-ol hydrobromide
Parent CAS No.
[78950-78-4]
Order
Size
Unit Price
Stock
10 mg
€50.00
In Stock | | axonmedchem |
| CM1 | Axon 2479
CAS [1643659-63-5]
MF C14H22N2O3MW 266.34
Purity:
100%
Soluble in water and DMSO
Description
Orally active iron chelator with high affinity and selectivity for iron(III) (relative metal complex stability constants of pFe(III)= 20.3; pCu(II)= 9.8; pZn(II)= 6.2) and a suit-able partition coefficient to permeate membranes. CM1 is able to penetrate hepatocytes and relatively non toxic. Potential therapeutic for patients suffering from thalassaemia related iron overload Moreover, CM1 shows an inhibitory effect on the growth of Plasmodium falciparum (malaria parrasite; IC50 value 35 µM).
KEYWORDS: CM1 | supplier | Iron chelator | CAS [1643659-63-5] | Iron (III) | FE(III) | Chelator | thalassaemia | hepatocytes | malaria | parasite | Plasmodium | | axonmedchem |
| KDU691 | Axon 2845
CAS [1513879-19-0]
MF C22H18ClN5O2MW 419.86
Purity:
99%
Soluble in DMSO
Description
KDU691 is a plasmodium PI4K inhibitor (IC50 values of 0.18 μM and 0.061 μM against hypnozoite forms and liver schizontsm, respectively) which selectively inhibits dihydroartemisinin-pretreated Plasmodium falciparum ring-stage parasites. Moreover, KDU691 was fully protective when administered in vivo as causal prophylactic and radical-cure agents for Plasmodium cynomolgi sporozoite-infected rhesus macaques.
KEYWORDS: KDU691 | supplier | PI4K inhibitor | KDU-691 | KDU 691 | CAS [1513879-19-0] | Phosphatidylinositol | PI4K | Inhibitor | Enzymes | Plasmodium | | axonmedchem |
| SMER 28 | Axon 2627
CAS [307538-42-7]
MF C11H10BrN3MW 264.12
Purity:
99%
Soluble in 0.1N HCl(aq) and DMSO
Description
Small molecule enhancer of rapamycin that enhances the clearance of mutant aggregate-prone proteins by autophagy in mammalian cell models of Huntington’s and Parkinson’s disease, independent of mTOR and Atg5 pathways. SMER28 also promotes reprogramming of fibroblasts (the conversion efficiency for adult tail-tip fibroblasts in particular) into neural stem cells, if combined with RG108 (Axon 1691) and Parnate.
KEYWORDS: SMER 28 | supplier | Autophagy inducer; SMER | SMER28 | SMER-28 | CAS [307538-42-7] | Small molecule enhancer of rapamycin | SMER | clearance | Huntington’s | Parkinson’s | reprogramming | fibroblasts | neural stem cells | | axonmedchem |
| Broxaldine - Brobenzoxaldine | Axon 2804
CAS [3684-46-6]
MF C17H11Br2NO2MW 421.08
Purity:
99%
Soluble in DMSO
Description
Broxaldine is an antiprotozoal drug.
KEYWORDS: Broxaldine | supplier | Antiprotozoal drug | Brobenzoxaldine | CAS [3684-46-6] | Non Selective | Non Selective | Antiprotozoal | Antiparasitic | | axonmedchem |
| VE 821 | Axon 1893
CAS [1232410-49-9]
MF C18H16N4O3SMW 368.41
Purity:
99%
Soluble in DMSO
Description
Potent and selective inhibitor of the DNA damage response (DDR) kinase ATR. which sensitises tumour cells to DNA damage induced by radiation or chemotoxic drugs, by disrupting the DNA damage checkpoint and inhibiting DNA repair.
KEYWORDS: VE 821 | supplier | ATR inhibitor | VE821 | VE-821 | CAS [1232410-49-9] | DNA-damage response | DDR | ATM | sensitization | radiation | chemotoxic | checkpoint | repair | | axonmedchem |
| Tenovin 6 - Tnv 6 | Axon 2249
CAS [1011557-82-6]
MF C25H34N4O2SMW 454.63
Purity:
99%
Soluble in 0.1N HCl(aq) and DMSO
Description
Small molecule, water soluble p53 activator and SIRT inhibitor (IC50 values of 21 μM, 10 μM, and 67 μM for purified human SIRT1, 2, and 3, respectively, in a peptide deacetylase assay). Tenovin 6 reduces chronic lymphocytic leukaemia (CLL) cell viability with dysregulation of autophagy, without increasing p53-pathway activity. It induces p53-dependent apoptosis in many malignant cells.
References
Certificates
Categories
Extra info
Lain S. et al. Discovery, in vivo activity, and mechanism of action of a small-molecule p53 activator. Cancer Cell. 2008, 13, 454-463.
Groves MJ et al. p53 and cell cycle independent dysregulation of autophagy in chronic lymphocytic leukaemia. Br. J. Cancer. 2013, 109, 2434-2444.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Cycle Regulation
Cell Signaling & Oncology
CNS
Diabetes & Metabolism
Epigenetics
p53
p53-Tumor Suppression
DNA-damage Response
EC 3.5.1.98
SIRT
Small water soluble p53 activator and SIRT inhibitor
Chemical name
4-tert-butyl-N-(4-(5-(dimethylamino)pentanamido)phenylcarbamothioyl)benzamide
Parent CAS No.
[1011557-82-6]
Order
Size
Unit Price
Stock
5 mg
€105.00
In Stock | | axonmedchem |
| A 66 | Axon 1831
CAS [1166227-08-2]
MF C17H23N5O2S2MW 393.53
Purity:
99%
Optical purity:
Optically pure
Soluble in DMSO
Description
Potent and specific PI3K p110α inhibitor (IC50: 32 nM); highly selective for p110α over other PI3Ks and having a high degree of specificity as it does not target other protein kinases tested; highly recommended tool in researching p110α isoform
References
Certificates
Categories
Extra info
S Jamieson et al. A drug targeting only p110α can block phosphoinositide 3-kinase signalling and tumour growth in certain cell types. Biochem J. 2011, 438(Pt 1), 53–62.
Ashley J. Waardenberg et al. Phosphoinositide 3-Kinase (PI3K(p110α)) Directly Regulates Key Components of the Z-disc and Cardiac Structure. J. Biol. Chem. 2011, 286, 30837-30846.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
PI3K
PI3K-Akt-mTOR
EC 2.7.1.153
PI3K inhibitor (p110-α specific)
Chemical name
(S)-N1-(2-tert-butyl-4'-methyl-4,5'-bithiazol-2'-yl)pyrrolidine-1,2-dicarboxamide
Parent CAS No.
[1166227-08-2]
Order
Size
Unit Price
Stock
5 mg
€95.00
In Stock | | axonmedchem |
| NVP-BKM120 - BKM 120 | Axon 1797
CAS [944396-07-0]
MF C18H21F3N6O2MW 410.39
Purity:
98%
Soluble in DMSO
Description
Potent, selective, orally bioavailable class I PI3K inhibitor
References
Certificates
Categories
Extra info
CW Lindsley et al. (3-Cyano-5-fluorophenyl)biaryl negative allosteric modulators of mGlu5: discovery of a new tool compound with activity in the OSS mouse model of addiction. ACS Chem. Neurosci. 2011, 2(8), 471-482.
D Koul et al. Antitumor activity of NVP-BKM120--a selective pan class I PI3 kinase inhibitor showed differential forms of cell death based on p53 status of glioma cells. Clin Cancer Res. 2012, 18(1), 184-195.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
PI3K
PI3K-Akt-mTOR
EC 2.7.1.153
Class I PI3K inhibitor
Chemical name
5-(2,6-dimorpholinopyrimidin-4-yl)-4-(trifluoromethyl)pyridin-2-amine
Parent CAS No.
[944396-07-0]
Order
Size
Unit Price
Stock
5 mg
€90.00
In Stock | | axonmedchem |
| DBeQ | Axon 1826
CAS [177355-84-9]
MF C22H20N4MW 340.42
Purity:
99%
Soluble in DMSO
Description
Potent, cell-permeable, selective and reversible p97 ATPase inhibitor; impairs both ubiquitin-dependent and autophagic protein clearance pathways and induces executioner caspases 3 and 7
References
Certificates
Categories
Extra info
TF Chou et al. Reversible inhibitor of p97, DBeQ, impairs both ubiquitin-dependent and autophagic protein clearance pathways. Proc. Natl. Acad. Sci. USA. 2011, 108(12), 4834-4839.
TF Chou and RJ Deshaies. Development of p97 AAA ATPase inhibitors. Autophagy. 2011, 7(9), 1091-1092.
Certificate of Analysis
Material Safety Data Sheet
Cell Cycle Regulation
Cell Signaling & Oncology
ATPase (p97)
Ubiquitin
EC 3.6.4.6
Inhibitor of p97 ATPase
Chemical name
N2,N4-dibenzylquinazoline-2,4-diamine
Parent CAS No.
[177355-84-9]
Order
Size
Unit Price
Stock
10 mg
€90.00
In Stock | | axonmedchem |
| D 106669 | Axon 1719
CAS [938444-93-0]
MF C17H18N6OMW 322.36
Purity:
98%
Soluble in DMSO
Description
Highly potent and selective PI3K inhibitor, selectively inhibiting class I PI3K (PI3Kα IC50 <10 nM, >3 log selectivity against tyrosine or serine/threonine kinases, except ERK1 and 2) and showed some activity in A549 (lung cancer) xenografts mouse model at oral dose of 30 mg/kg twice daily
References
Certificates
Categories
Extra info
SM Maira et al. Discovery of novel anticancer therapeutics targeting the PI3K/Akt/mTOR pathway. Future Med. Chem. 2009, 1(1), 137-155.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
PI3K
PI3K-Akt-mTOR
EC 2.7.1.153
Potent and selective PI3K inhibitor
Chemical name
1-ethyl-3-(3-(p-tolylamino)pyrido[2,3-b]pyrazin-6-yl)urea
Parent CAS No.
[938444-93-0]
Order
Size
Unit Price
Stock
2 mg
€85.00
In Stock | | axonmedchem |
| KU 0060648 trihydrochloride | Axon 1584
CAS [881375-00-4]
MF C33H34N4O4S.3HClMW 692.10
Purity:
99%
Soluble in water and DMSO
Description
Potent and selective inhibitor of DNA-dependent protein kinase (DNA-PK), (IC50 = 8.6 nM); with 20-1000 fold selectivity for DNA-PK over other PIKKs and a panel of 60 kinases. Product is discontinued (Autumn 2016).
* The parent molecule of KU 0060648 (Axon 2604) is available online, and makes an excellent alternative for Axon 1584.
KEYWORDS: KU 0060648 trihydrochloride | supplier | DNA-PK inhibitor | KU0060648 HCl | CAS [881375-00-4] | DNA-RNA | DNA-PK | Inhibitor | PIKK | PI3K | cancer | DNA repair | DSB | double-strand breaks | | axonmedchem |
| CP 466722 | Axon 1495
CAS [1080622-86-1]
MF C17H15N7O2MW 349.35
Purity:
99%
Soluble in DMSO
Description
Specific ATM inhibitor; no inhibition of PI3K or PI3K-like protein kinases (PIKK) or Abl kinase in cells; does inhibit cellular ATM-dependent phosphorylation events and disruption of ATM function resulted in characteristic cell cycle checkpoint defects; highly recommended tool to rapidly and reversibly regulate ATM activity.
KEYWORDS: CP 466722 | supplier | ATM inhibitor | CP466722 | CP-466722 | CAS [1080622-86-1] | DNA-RNA | DNA damage | cell cycle | checkpoint | ataxia-telangiectasia | radiosensitization | | axonmedchem |
| NVP-BBD130 - BBD 130 | Axon 1520
CAS [853910-61-9]
MF C28H21N5OMW 443.50
Purity:
99%
Moderately soluble in DMSO
Description
Orally potent and selective dual PI3K/mTOR inhibitor; IC50 values to be 72, 2336, 201 and 382 nM for PI3K p110 α, β, δ and γ isoforms, respectively; inhibition of PI3K/mTOR pathway like NVP-BEZ235, BBD130 efficiently attenuates growth and proliferation of melanoma primary tumors and metastasis
References
Certificates
Categories
Extra info
R Marone et al. Targeting Melanoma with Dual Phosphoinositide 3-Kinase/Mammalian Target of Rapamycin Inhibitors. Mol. Cancer Res. 2009, 7(4), 601-613.
F Stauffer et al. Imidazo[4,5-c]quinolines as inhibitors of the PI3K/PKB-pathway. Bioorg. Med. Chem. Lett. 2008, 18, 1027-1030.
SM Maria, P Furet and F Stauffer. Discovery of novel anticancer therapeutics targeting the PI3K/Akt/mTOR pathway. Future Med. Chem. 2009, 1(1), 137-155.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
PI3K
PI3K-Akt-mTOR
EC 2.7.1.153
Dual PI3K and mTOR kinase inhibitor
Chemical name
2-Methyl-2-[4-(3-methyl-2-oxo-8-pyridin-3ylethynyl-2,3-dihydro-imidazo[4,5-c]quinolin-1-yl)-phenyl]-propionitrile
Parent CAS No.
[853910-61-9]
Order
Size
Unit Price
Stock
5 mg
€125.00
In Stock | | axonmedchem |
| AS 252424 | Axon 1424
CAS [900515-16-4]
MF C14H8FNO4SMW 305.28
Purity:
99%
Soluble in 0.1N NaOH(aq) and DMSO
Description
Potent and selective PI3K p110γ inhibitor; IC50 values for inhibition of human recombinant PI3Kγ, α, β, and δ are 30, 940, 20,000, and 20,000 nM respectively. A water-soluble bispotassium salt form of AS 252424 is available as well (Axon 1436).
References
Certificates
Categories
Extra info
V Pomel et al. Furan-2-ylmethylene thiazolidinediones as novel, potent, and selective inhibitors of phosphoinositide 3-kinase gamma. J. Med. Chem. 2006, 49, 3857-3871.
T Rückle et al. PI3Kγ inhibition: Towards an 'aspirin of the 21st century'?. Nature Reviews Drug Discovery 2006, 5, 903-918.
BT Hennessy et al. Exploiting the PI3K/AKT pathway for cancer drug discovery.Nat. Rev. Drug Discov. 2005,4, 988-1004.
AM Condliffe et al. Sequential activation of class IB and class IA PI3K is important for the primed respiratory burst of human but not murine neutrophils. Blood 2005, 106, 1432-1440.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
PI3K
PI3K-Akt-mTOR
EC 2.7.1.153
PI3K inhibitor (p110-γ specific)
Chemical name
5-[1-[5-(4-Fluoro-2-hydroxy-phenyl)-furan-2-yl]-meth-(Z)-ylidene]-thiazolidine-2,4-dione
Parent CAS No.
[900515-16-4]
Order
Size
Unit Price
Stock
5 mg
€85.00
In Stock | | axonmedchem |
| NU 7441 - KU 47788 | Axon 1463
CAS [503468-95-9]
MF C25H19NO3SMW 413.49
Purity:
99%
Soluble in DMSO
Description
Potent, selective and ATP-competitive inhibitor of DNA-dependent protein kinase (DNA-PK), with IC50 value to be 13 nM for in vitro DNA-PK inhibition; selectivity >100 fold for DNA-PK over related kinases.
KEYWORDS: NU 7441 | supplier | DNA-PK inhibitor | KU 47788 | NU7441 | KU47788 | CAS [503468-95-9] | DNA-RNA | protein kinase | double-strand break | DSB | ATP-competitive | topoisomerase | cell cycle arrest | | axonmedchem |
| PI 103 hydrochloride | Axon 1380
CAS [371935-79-4]
MF C19H16N4O3.HClMW 384.82
Purity:
99%
Soluble in DMSO
Description
A selective class I PI3K inhibitor; it inhibits PI3K p110 isoforms, mTOC1 and also DNA-PK; a valuable tool compound
References
Certificates
Categories
Extra info
ZA Knight et al. A Pharmacological Map of the PI3-K Family Defines a Role for p110α in Insulin Signaling. Cell 2006, 125, 733–747.
FI Raynaud et al. Pharmacologic characterization of a potent inhibitor of class I phosphatidylinositide 3-kinases. Cancer Res. 2007, 67(12), 5840-50.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
PI3K
PI3K-Akt-mTOR
EC 2.7.1.153
PI3K inhibitor (p110 specific)
Chemical name
3-[4-(4-morpholinyl)pyrido[3',2':4,5]furo[3,2-d]pyrimidin-2-yl]-phenol hydrochloride
Parent CAS No.
[371935-74-9]
Order
Size
Unit Price
Stock
2 mg
€60.00
In Stock | | axonmedchem |
| TGX 221 | Axon 1417
CAS [663619-89-4]
MF C21H24N4O2MW 364.44
Purity:
99%
Soluble in DMSO
Description
Potent and specific PI3K p110β inhibitor
References
Certificates
Categories
Extra info
SP Jackson et al. PI 3-kinase p110b: A new target for antithrombotic therapy. Nature Medicine 2005, 11(5), 507-514.
BT Hennessy et al. Exploiting the PI3K/AKT pathway for cancer drug discovery. Nature Reviews Drug Discovery 2005, 4988-1004.
AM Condliffe et al. Sequential activation of class IB and class IA PI3K is important for the primed respiratory burst of human but not murine neutrophils. Blood 2005, 106, 1432-1440.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
PI3K
PI3K-Akt-mTOR
EC 2.7.1.153
PI3K inhibitor (p110 β specific)
Chemical name
7-methyl-2-morpholin-4-yl-9-(1-phenylaminoethyl)-pyrido[1,2-a]-pyrimidin-4-one
Parent CAS No.
[663619-89-4]
Order
Size
Unit Price
Stock
2 mg
€70.00
In Stock | | axonmedchem |
| KU 55933 | Axon 1367
CAS [587871-26-9]
MF C21H17NO3S2MW 395.49
Purity:
99%
Soluble in DMSO
Description
Potent, ATP-competitive and selective ATM inhibitor (Ki = 2.2 nM, IC50 = 13 nM)
References
Certificates
Categories
Extra info
I Hickson et al. Identification and Characterization of a Novel and Specific Inhibitor of the Ataxia-Telangiectasia Mutated Kinase ATM. Cancer Res. 2004, 64, 9152.
A Lau et al. Suppression of HIV-1 infection by a small molecule inhibitor of the ATM kinase. Nat. Cell Biol. 2005, 7, 493-500.
Y Li and DQ Yang. The ATM Inhibitor KU-55933 Suppresses Cell Proliferation and Induces Apoptosis by Blocking Akt In Cancer Cells with Overactivated Akt. Mol. Cancer Ther. 2010, 9, 113.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Cycle Regulation
Cell Signaling & Oncology
ATM
p53-Tumor Suppression
PI3K-Akt-mTOR
DNA-damage Response
EC 2.7.11.1
ATM inhibitor
Chemical name
2-Morpholin-4-yl-6-thianthren-1-yl-pyran-4-one
Parent CAS No.
[587871-26-9]
Order
Size
Unit Price
Stock
10 mg
€125.00
In Stock | | axonmedchem |
| GDC 0941 bismesylate - Pictilisib | Axon 1377
CAS [957054-33-0]
MF C23H27N7O3S2.2CH4O3SMW 705.85
Purity:
99%
Soluble in water and DMSO
Description
Potent, selective, orally bioavailable inhibitor of class I PI3 kinase (PI3K) under clinical trials, with IC50 values (nM) of 3, 33, 3, 75, 1230 and 580 for p110 α, β, δ and γ isoforms, DNA-PK and mTOR; water-soluble form.
KEYWORDS: GDC 0941 bismesylate | supplier | PI3K inhibitor | Pictilisib | GDC0941 | GDC-0941 | CAS [957054-33-0] | [957054-30-7] | Phosphatidylinositol | orally bioavailable | p110-alpha | DNA-PK | mTOR | water-soluble | | axonmedchem |
| PIK 90 | Axon 1362
CAS [677338-12-4]
MF C18H17N5O3MW 351.36
Purity:
99%
Moderately soluble in DMSO with 0.1N HCl(aq)
Description
Potent and cell permeable PI3K inhibitor, with IC50 values (nM) of 11, 350, 18, and 58 for p110 α, β, γ and δ isoforms, low mTOR activity.
KEYWORDS: PIK 90 | supplier | PI3K p110α inhibitor | PIK90 | PIK-90 | CAS [677338-12-4] - [677338-13-5] | | axonmedchem |
| LY 294002 | Axon 1366
CAS [154447-36-6]
MF C19H17NO3MW 307.34
Purity:
99%
Soluble in DMSO
Description
Potent and specific PI3K inhibitor
References
Certificates
Categories
Extra info
MH Cardone et al. Regulation of Cell Death Protease Caspase-9 by Phosphorylation. Science 1998, 282, 1318.
CJ Vlahos et al. A specific inhibitor of phosphatidylinositol 3-kinase, 2-(4-morpholinyl)-8-phenyl-4H-1-benzopyran-4-one (LY294002). J. Biol. Chem. 1994,269, 5241-5248.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Stem Cell
PI3K
PI3K-Akt-mTOR
EC 2.7.1.153
PI3K inhibitor
Chemical name
2-Morpholin-4-yl-8-phenyl-chromen-4-one
Parent CAS No.
[154447-36-6]
Order
Size
Unit Price
Stock
5 mg
€70.00
In Stock | | axonmedchem |
| BAG 956 - NVP-BAG956 | Axon 1282
CAS [853910-02-8]
MF C28H21N5MW 427.50
Purity:
99%
Soluble in DMSO
Description
Potent, ATP-competitive and selective dual PI3K and PDPK1 inhibitor in vitro and in vivo, with IC50 values to be 56, 444, 34, 117 and 240 nM for PI3K p110 α, β, δ and γ and PDPK1 kinases, respectively
References
Certificates
Categories
Extra info
R Marone et al. Targeting Melanoma with Dual Phosphoinositide 3-Kinase/Mammalian Target of Rapamycin Inhibitors. Mol. Cancer Res. 2009, 7(4), 601-613.
SM Maria, P Furet and F Stauffer. Discovery of novel anticancer therapeutics targeting the PI3K/Akt/mTOR pathway. Future Med. Chem. 2009, 1(1), 137-155.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
PI3K
PI3K-Akt-mTOR
EC 2.7.1.153
PDPK
PI3K and PDPK1 inhibitor
Chemical name
2-methyl-2-[4-(2-methyl-8-pyridin-3-ylethynyl-imidazo[4,5-c]quinolin-1-yl)-phenyl]-propionitrile
Parent CAS No.
[853910-02-8]
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Size
Unit Price
Stock
5 mg
€95.00
In Stock | | axonmedchem |
| GMC 1-161 | Axon 2851
CAS [95316-97-5]
MF C19H22N4OMW 322.40
Purity:
99%
Soluble in 0.1N HCl(aq) and DMSO
Description
Analogue of clozapine (Axon 1146); devoid of affinity for the DA D1 receptor, but with affinities at 5-HT2A/2C, hM1 and DA D2 receptors.
KEYWORDS: GMC 1-161 | supplier | Clozapine analogue | GMC1-161 | GMC1161 | CAS [95316-97-5] | Serotonin | 5-HT2A | 5-HT2C | CHRM1 | D2 | Agonist | Receptors | | axonmedchem |
| PIK 75 hydrochloride | Axon 1334
CAS [945619-31-8]
MF C16H14BrN5O4SMW 452.28
Purity:
99%
Moderately soluble in DMSO
Description
PI3K p110α specific inhibitor; IC50 values (nM): 7.8 (p110α), 343 (p110β), 907 (p110δ) (Chaussade et al reported).
KEYWORDS: PIK 75 hydrochloride | supplier | PI3K p110α inhibitor | PIK75 HCl | PIK-75 | CAS [945619-31-8] | [372196-77-5] | Phosphatidylinositol | PI3K | p110-alpha | insulin signaling | | axonmedchem |
| SB 242084 hydrochloride | Axon 1745
CAS [1260505-34-7]
MF C21H19ClN4O2.HClMW 431.32
Purity:
99%
Soluble in DMSO
Description
Selective and brain penetrant 5-HT2C receptor antagonist
References
Certificates
Categories
Extra info
SM Bromidge et al. 6-Chloro-5-methyl-1-[[(2-methyl-3-pyridyl)oxy]-5-pyridyl]carbamoyl]-indoline (SB-242084): the first selective and brain penetrant 5-HT2C receptor antagonist. J. Med. Chem. 1997, 40(22), 3494-3496.
GA Kennet et al. SB 242084, a selective and brain penetrant 5-HT2C receptor antagonist. Neuropharmacology 1997, 36(4-5), 609-620.
GL Dalton et al. Serotonin 1B and 2C receptor interactions in the modulation of feeding behaviour in the mouse. Psychopharmacol. 2006, 185(1), 45-57.
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CNS
5-HT2C
A17
Selective 5-HT2C receptor antagonist
Chemical name
6-chloro-5-methyl-N-(6-(2-methylpyridin-3-yloxy)pyridin-3-yl)indoline-1-carboxamide hydrochloride
Parent CAS No.
[181632-25-7]
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Size
Unit Price
Stock
5 mg
€90.00
In Stock | | axonmedchem |
| Clozapine, N-Desmethyl- - Norclozapine | Normethylclozapine | ACP-104 | Axon 2846
CAS [6104-71-8]
MF C17H17ClN4MW 312.80
Purity:
99%
Soluble in 0.1N HCl(aq) and DMSO
Description
Major metabolite of Clozapine (Axon 1146). N-Desmethylclozapine is a relatively potent and efficacious partial agonist at the D2 and D3 dopamine receptors, while showing inverse agonism at the 5-HT2A receptor. Moreover, N-Desmethylclozapine is a potent partial agonist at the muscarinic M1 receptor and a selective agonist at δ opioid receptor.
KEYWORDS: N-Desmethylclozapine | supplier | Clozapine metabolite | Norclozapine | Normethylclozapine | ACP-104 | ACP104 | ACP 104 | CAS [6104-71-8] | Serotonin; Dopamine | D (Non Selective) | 5-HT (Non Selective) | Agonist | Receptors | Muscarinic M1 | δ Opioid | | axonmedchem |
| Ketanserin - R 41468 | Axon 1450
CAS [74050-98-9]
MF C22H22FN3O3MW 395.43
Purity:
99%
Soluble in water and DMSO
Description
5-HT2A receptor antagonist; an antihypertensive; with tritium (3H) radioactively labeled ketanserin is used as a radioligand for the serotonin 5-HT2A receptor, e.g. in receptor binding assays and autoradiography
References
Certificates
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Extra info
A. Pazos et al. Serotonin receptors in the Human Brain—IV. Autoradiographic mapping of serotonin-2 receptors. Neuroscience 1987, 21(1), 123–139.
L Sharon et al.. Expression of serotonin 5-HT2A receptors in the human cerebellum and alterations in schizophrenia. Synapse 2001, 42(2), 104–114.
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Material Safety Data Sheet
CNS
5-HT2A
A17
5-HT2A antagonist
Chemical name
3-{2-[4-(4-Fluoro-benzoyl)-piperidin-1-yl]-ethyl}-1H-quinazoline-2,4-dione
Parent CAS No.
[74050-98-9]
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Size
Unit Price
Stock
10 mg
€55.00
In Stock | | axonmedchem |
| Agomelatine | Axon 1492
CAS [138112-76-2]
MF C15H17NO2MW 243.30
Purity:
99%
Soluble in DMSO
Description
Potent melatonin agonist; first melatonin antidepressant; also known as a norepinephrine dopamine disinhibitor (NDDI) due to its antagonism of the 5-HT2C receptor
References
Certificates
Categories
Extra info
SA Montgomery. Major depressive disorders: clinical efficacy and tolerability of agomelatine, a new melatonergic agonist. Eur. Neuropsychopharmacol, 2006, 16, suppl 5, S633-S638.
MJ Millan et al. The novel melatonin agonist agomelatine (S20098) is an antagonist at 5-HT2C receptors, blockade of which enhances the activity of frontocortical dopaminergic and adrenergic pathways. J. Pharmacol. Exp. Ther. 2003, 306 (3), 954–954.
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Material Safety Data Sheet
CNS
5-HT2C
MT2
A9
MT1
Melatonin agonist; 5-HT2C antagonist
Chemical name
N-[2-(7-methoxynaphthalen-1-yl)ethyl]acetamide
Parent CAS No.
[138112-76-2]
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Size
Unit Price
Stock
10 mg
€75.00
In Stock | | axonmedchem |
| Clozapine N-oxide - CNO | Axon 2796
CAS [34233-69-7]
MF C18H19ClN4OMW 342.82
Purity:
99%
Soluble in water and DMSO
Description
Metabolite of the atypical antipsychotic agent Clozapine (Axon 1146). Muscarinic DREADD (designer receptor exclusively activated by a designer drug) agonist.
KEYWORDS: Clozapine N-oxide | supplier | DREADD agonist | CNO | CAS [34233-69-7] | Acetylcholine | DREADD | Agonist | Receptors | Muscarinic | | axonmedchem |
| GMC 1-109 | Axon 1289
CAS [183140-96-7]
MF C19H19F3N4O3SMW 440.44
Purity:
98%
Soluble in 0.1N HCl(aq) and DMSO
Description
Analogue of clozapine (Axon 1146); devoid of DA, 5-HT2, H1 and α1 affinities, but with high M1 affinity (IC50 value of 35 nM).
KEYWORDS: GMC 1-109 | supplier | Clozapine analog | GMC1-109 | GMC1109 | CAS [183140-96-7] | Axon Medchem | Axon 1289 | Acetylcholine | CHRM1 | Antagonist | Receptors | Muscarinic | | axonmedchem |
| Eplivanserin - SR 46349B | Axon 1439
CAS [130580-02-8]
MF C19H21FN2O2.½C4H4O4MW 386.42
Purity:
99%
Soluble in DMSO
Description
Potent, selective and p.o. active 5-HT2A antagonist; functionally also an inverse agonist of 5-HT2A receptor; no affinity to dopamine, histamine and adrenergic receptors; therapeutic agent for the treatment of insomnia
References
Certificates
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Extra info
M. Rinaldi-Carmona et al. Biochemical and Pharmacological Properties of SR 46349B, a New Potent and Selective 5-Hydroxytryptamine2 Receptor Antagonist. JPET 1992, 262(2), 759-768.
F Chaouloff et al. Repeated DOI and SR 46349B treatments do not affect elevated plus-maze anxiety despite opposite effects on cortical 5-HT2A receptors. Eur. J. Pharmacol. 1997, 334(1), 25-29.
BR Teergarden et al. 5-HT2A Inverse-Agonists for the Treatment of Insomnia. Current Topics Med. Chem. 2008, 8(11), 969–976.
Certificate of Analysis
Material Safety Data Sheet
CNS
5-HT2A
A17
5-HT2A antagonist/inverse agonist
Chemical name
(E)-1-(2-Fluoro-phenyl)-3-(4-hydroxy-phenyl)-propenone O-(2-dimethylamino-ethyl)-oxime hemi-fumarate
Parent CAS No.
[130579-75-8]
Order
Size
Unit Price
Stock
5 mg
€80.00
In Stock | | axonmedchem |
| Luzindole - N 0774 | Axon 1350
CAS [117946-91-5]
MF C19H20N2OMW 292.37
Purity:
99%
Soluble in DMSO
Description
A putative melatonin antagonist
References
Certificates
Categories
Extra info
C Browning et al., Pharmacological characterization of human recombinant melatonin MT(1) and MT(2) receptors. Br. J. Pharmacol. 2000, 129, 877-886.
ML Dubocovich. Luzindole (N-0774): a novel melatonin receptor antagonist. J. Pharmacol. Exp. Ther. 1988, 246, 902-910.
M Zhou et al. Luzindole, a melatonin receptor antagonist, inhibits the transient outward K+ current in rat cerebellar granule cells. Brain Res. 2003, 970, 169-177.
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Material Safety Data Sheet
CNS
MT2
A9
MT1
Melatonin antagonist
Chemical name
N-[2-(2-Benzyl-1H-indol-3-yl)-ethyl]-acetamide
Parent CAS No.
[117946-91-5]
Order
Size
Unit Price
Stock
10 mg
€95.00
In Stock | | axonmedchem |
| DH 97 | Axon 1351
CAS [343263-95-6]
MF C22H26N2OMW 334.45
Purity:
99%
Soluble in DMSO
Description
Melatonin antagonist; MT2 selective
References
Certificates
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Extra info
MT Teh & D Sugden. Comparison of the structure-activity relationships of melatonin receptor agonists and antagonists: lengthening the N-acyl side-chain has differing effects on potency on Xenopus melanophores. N. S. Arch. Pharmacol. 1998, 358, 522.
KN Ting et al. Molecular and pharmacological evidence for MT1 melatonin receptor subtype in the tail artery of juvenile Wistar rats. Br. J. Pharmacol. 1999, 127, 987.
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Material Safety Data Sheet
CNS
MT2
A9
Melatonin (MT2) antagonist
Chemical name
Pentanoic acid [2-(2-benzyl-1H-indol-3-yl)-ethyl]-amide
Parent CAS No.
[343263-95-6]
Order
Size
Unit Price
Stock
10 mg
€95.00
In Stock | | axonmedchem |
| AH 002 - M-PDOT, 8- | Axon 1336
CAS [134865-70-6]
MF C14H19NO2MW 233.31
Purity:
98%
Soluble in DMSO
Description
Melatonin agonist; less potent in comparison with AH-001 (Axon 1335), but more selective on MT2 vs MT1
References
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Extra info
Browning et al. Pharmacological characterization of human recombinant melatonin MT1 and MT2 receptors. Br. J. Pharmacol. 2000, 129, 877.
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CNS
MT2
A9
Melatonin agonist
Chemical name
N-(8-Methoxy-1,2,3,4-tetrahydro-naphthalen-2-yl)-propionamide
Parent CAS No.
[134865-70-6]
Order
Size
Unit Price
Stock
10 mg
€80.00
In Stock | | axonmedchem |
| AH 001 - M-ADOT, 8- | Axon 1335
CAS [80270-68-4]
MF C13H17NO2MW 219.28
Purity:
98%
Soluble in DMSO
Description
Potent melatonin agonist
References
Certificates
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Extra info
WJ Drijfhout et al. Novel non-indolic melatonin receptor agonists differentially entrain endogenous melatonin rhythm and increase its amplitude. Eur. J. Pharmacol. 1999, 382, 157-166.
ML Dubocovich et al. Melatonin receptor antagonists that differentiate between the human Mel1a and Mel1b recombinant subtypes are used to assess the profile of the rabbit retina ML1 presynaptic heteroreceptor. N.S. Arch. Pharmacol. 1997, 355, 365-375.
Certificate of Analysis
Material Safety Data Sheet
CNS
MT2
A9
MT1
Melatonin agonist
Chemical name
N-(8-Methoxy-1,2,3,4-tetrahydro-naphthalen-2-yl)-acetamide
Parent CAS No.
[80270-68-4]
Order
Size
Unit Price
Stock
10 mg
€80.00
In Stock | | axonmedchem |
| MDL 105725, (-)- | Axon 1108
CAS [311348-81-9]
MF C21H26FNO3MW 359.43
Purity:
98%
Optical purity:
98% ee
Soluble in DMSO and Ethanol
Description
Less active metabolite of MDL 100907 (Axon 1105), a selective 5-HT2A antagonist; Precursor for [11C]MDL100907
References
Certificates
Categories
Extra info
T Ullrich and KC Rice. A practical synthesis of the serotonin 5-HT2a receptor antagonist mdl 100907, its enantiomer and their 3-phenolic derivatives as precursors for [11c]labeled pet ligands. Bioorg. Med. Chem. 2000, 8(10), 2427-2432.
J H Kehne et al. Effects of the Selective 5-HT2A Receptor Antagonist MDL 100,907 on MDMA-Induced Locomotor Stimulation in Rats.Neuropsychopharmacol. 1996, 15, 116-124.
Certificate of Analysis
Material Safety Data Sheet
CNS
5-HT2A
A17
5-HT2A antagonist
Chemical name
3-((S)-{1-[2-(4-Fluoro-phenyl)-ethyl]-piperidin-4-yl}-hydroxy-methyl)-2-methoxy-phenol
Parent CAS No.
[311348-81-9]
Inquire | | axonmedchem |
| MDL 105725, (+)- - MDL 105725 | Axon 1107
CAS [189192-18-5]
MF C21H26FNO3MW 359.43
Purity:
99%
Optical purity:
98% ee
Soluble in DMSO
Description
Active metabolite of MDL 100907 (Axon 1104), a selective 5-HT2A antagonist; Precursor for [11C]MDL100907
References
Certificates
Categories
Extra info
T Ullrich and KC Rice. A practical synthesis of the serotonin 5-HT2a receptor antagonist mdl 100907, its enantiomer and their 3-phenolic derivatives as precursors for [11c]labeled pet ligands. Bioorg. Med. Chem. 2000, 8(10), 2427-2432.
J H Kehne et al. Effects of the Selective 5-HT2A Receptor Antagonist MDL 100,907 on MDMA-Induced Locomotor Stimulation in Rats.Neuropsychopharmacol. 1996, 15, 116-124.
Y Huang et al. An efficient synthesis of the precursors of [11C]MDL100907 labeled in two specific positions. J. Labelled Compd. Radiopharm. 1999, 42, 949-957.
DO Scott and TG Heath. Investigation of the CNS penetration of a potent 5-HT2A receptor antagonist (MDL 100,907) and an active metabolite (MDL 105,725) using in vivo microdialysis sampling in the rat. J. Pharm. Biomed Anal. 1998, 17(1), 17-25.
Certificate of Analysis
Material Safety Data Sheet
CNS
5-HT2A
A17
5-HT2A antagonist
Chemical name
3-((R)-{1-[2-(4-Fluoro-phenyl)-ethyl]-piperidin-4-yl}-hydroxy-methyl)-2-methoxy-phenol
Parent CAS No.
[189192-18-5]
Order
Size
Unit Price
Stock
1 mg
€85.00
In Stock | | axonmedchem |
| MDL 105725, (±)- | Axon 1106
CAS [1018473-89-6]
MF C21H26FNO3MW 359.43
Purity:
99%
Soluble in DMSO
Description
Active metabolite of MDL 100907
References
Certificates
Categories
Extra info
T Ullrich and KC Rice. A practical synthesis of the serotonin 5-HT2a receptor antagonist mdl 100907, its enantiomer and their 3-phenolic derivatives as precursors for [11c]labeled pet ligands. Bioorg. Med. Chem. 2000, 8(10), 2427-2432.
J H Kehne et al. Effects of the Selective 5-HT2A Receptor Antagonist MDL 100,907 on MDMA-Induced Locomotor Stimulation in Rats.Neuropsychopharmacol. 1996, 15, 116-124.
Certificate of Analysis
Material Safety Data Sheet
CNS
5-HT2A
A17
5-HT2A antagonist
Chemical name
3-({1-[2-(4-Fluoro-phenyl)-ethyl]-piperidin-4-yl}-hydroxy-methyl)-2-methoxy-phenol
Parent CAS No.
[1018473-89-6]
Order
Size
Unit Price
Stock
10 mg
€145.00
In Stock | | axonmedchem |
| MDL 100009 - MDL 100907, (S)-(-)- | Axon 1105
CAS [175673-57-1]
MF C22H28FNO3MW 373.46
Purity:
99%
Optical purity:
98% ee
Soluble in DMSO and Ethanol
Description
S-enantiomer of MDL 100151 (Axon 1103); opposite enantiomer of MDL 100907 (Axon 1104), selective 5-HT2A antagonist
References
Certificates
Categories
Extra info
T Ullrich and KC Rice. A practical synthesis of the serotonin 5-HT2a receptor antagonist mdl 100907, its enantiomer and their 3-phenolic derivatives as precursors for [11c]labeled pet ligands. Bioorg. Med. Chem. 2000, 8(10), 2427-2432.
J H Kehne et al. Effects of the Selective 5-HT2A Receptor Antagonist MDL 100,907 on MDMA-Induced Locomotor Stimulation in Rats.Neuropsychopharmacol. 1996, 15, 116-124.
Certificate of Analysis
Material Safety Data Sheet
CNS
5-HT2A
A17
5-HT2A antagonist
Chemical name
(S)-(2,3-Dimethoxy-phenyl)-{1-[2-(4-fluoro-phenyl)-ethyl]-piperidin-4-yl}-methanol
Parent CAS No.
[175673-57-1]
Order
Size
Unit Price
Stock
5 mg
€125.00
In Stock | | axonmedchem |
| MDL 100151 - MDL 100907, (±)- | Axon 1103
CAS [139290-69-0]
MF C22H28FNO3MW 373.46
Purity:
99%
Soluble in DMSO and Ethanol
Description
Selective 5-HT2A antagonist; rac-M 100907, its more active enantiomer is (+)-MDL 100907 (Axon 1104); Reference standard for [11C]MDL100907 in PET/SPECT study
References
Certificates
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Extra info
HO Kalkman et al. Cataleptogenic effect of subtype selective 5-HT receptor antagonists in the rat. Eur. J. Pharmacol. 1998, 343(2-3), 201-7.
J H Kehne et al. Effects of the Selective 5-HT2A Receptor Antagonist MDL 100,907 on MDMA-Induced Locomotor Stimulation in Rats.Neuropsychopharmacol. 1996, 15, 116-124.
C Sanchez et al. In-vivo assessment of 5-HT2A and 5-HT2C antagonistic properties of newer antipsychotics. Behav. Pharmacol. 2000, 11, 291-98.
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Material Safety Data Sheet
CNS
5-HT2A
A17
5-HT2A antagonist
Chemical name
(2,3-Dimethoxy-phenyl)-{1-[2-(4-fluoro-phenyl)-ethyl]-piperidin-4-yl}-methanol
Parent CAS No.
[139290-69-0]
Order
Size
Unit Price
Stock
10 mg
€110.00
In Stock | | axonmedchem |
| MDL 100907 - Volinanserin | MDL 100907, (R)-(+)- | Axon 1104
CAS [139290-65-6]
MF C22H28FNO3MW 373.46
Purity:
99%
Optical purity:
98% ee
Soluble in DMSO and Ethanol
Description
A highly selective 5-HT2A antagonist, more active enantiomer of MDL 100151 (Axon 1103) in comparison with S-(-)-enantiomer (Axon 1105); a highly recommended tool compound in researching into 5-HT2A receptors
References
Certificates
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Extra info
SM Sorensen et al. Characterization of the 5-HT2 receptor antagonist MDL 100907 as a putative atypical antipsychotic: behavioral, electrophysiological and neurochemical studies. JPET 1993, 266(2), 684-691.
J H Kehne et al. Effects of the Selective 5-HT2A Receptor Antagonist MDL 100,907 on MDMA-Induced Locomotor Stimulation in Rats.Neuropsychopharmacol. 1996, 15, 116-124.
T de Paulis. M-100907 (Aventis). Curr Opin Investig Drugs. 2001, 2(1), 123-32.
GB Vary et al. M100907, a serotonin 5-HT2A receptor antagonist and putative antipsychotic, blocks dizocilpine-induced prepulse inhibition deficits in Sprague-Dawley and Wistar rats. Neuropsychopharmacol. 1999, 20(4), 311-21.
RY Wang and X Liang. M100907 and Clozapine, but not Haloperidol or Raclopride, Prevent Phencyclidine-Induced Blockade of NMDA Responses in Pyramidal Neurons of the Rat Medial Prefrontal Cortical Slice. Neuropsychopharmacol. 1998, 19, 74-85.
Certificate of Analysis
Material Safety Data Sheet
CNS
5-HT2A
A17
5-HT2A antagonist
Chemical name
(R)-(2,3-Dimethoxy-phenyl)-{1-[2-(4-fluoro-phenyl)-ethyl]-piperidin-4-yl}-methanol
Parent CAS No.
[139290-65-6]
Order
Size
Unit Price
Stock
5 mg
€110.00
In Stock | | axonmedchem |
| GMC 2-118 | Axon 1084
CAS [256227-78-8]
MF C29H31N5O5SMW 561.65
Purity:
98%
No solubility data
Description
Selective 5-HT1B antagonist, very potent 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.
CNS
5-HT1B
A19
5-HT1B antagonist
Chemical name
Methanesulfonic acid 4-{[2'-methyl-4'-(5-methyl-[1,3,4]oxadiazol-2-yl)-biphenyl-4-carbonyl]-amino}-2-(4-methyl-piperazin-1-yl)-phenyl ester
Parent CAS No.
[256227-78-8]
Order
Size
Unit Price
Stock
10 mg
€155.00
In Stock | | axonmedchem |
| 25CN-NBOH hydrochloride - NBOH-2C-CN hydrochloride | Axon 2811
CAS [1539266-32-4]
MF C18H20N2O3.HClMW 348.82
Purity:
98%
Soluble in water and DMSO
Description
25CN-NBOH is a highly selective and brain penetrant 5-HT2A receptor agonist (Ki value of 1.3 nM; EC50 value of 2.1 nM). Moreover, 25CN-NBOH was behaviorally active in two mouse models of hallucinogenic effects.
KEYWORDS: 25CN-NBOH hydrochloride | supplier | 5-HT2A agonist | NBOH-2C-CN hydrochloride | 25CN NBOH hydrochloride | 25CNNBOH hydrochloride | CAS [1539266-32-4] | [1391489-32-9] | Serotonin | 5-HT2A | Agonist | Receptors | | axonmedchem |
| Nefazodone hydrochloride - BMY 13754 | Axon 1102
CAS [82752-99-6]
MF C25H32ClN5O2.HClMW 506.47
Purity:
99%
Soluble in DMSO
Description
Antidepressant; It operates by blocking post-synaptic 5-HT2A receptors and, to a lesser extent, by inhibiting pre-synaptic serotonin and norepinephrine (noradrenaline) reuptake.
Nefazodone is also a relatively potent α1 adrenoceptor antagonist
References
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Certificate of Analysis
Material Safety Data Sheet
CNS
5-HT2A
A17
Antidepressant; 5-HT2A antagonist
Chemical name
2-{3-[4-(3-Chloro-phenyl)-piperazin-1-yl]-propyl}-5-ethyl-4-(2-phenoxy-ethyl)-2,4-dihydro-[1,2,4]triazol-3-one hydrochloride
Parent CAS No.
[83366-66-9]
Order
Size
Unit Price
Stock
10 mg
€85.00
In Stock | | axonmedchem |
| Flibanserin - BIMT 17 | Axon 1499
CAS [167933-07-5 ]
MF C20H21F3N4OMW 390.40
Purity:
99%
Soluble in DMSO
Description
A 5-HT1A receptor full agonist with 5-HT2A receptor antagonistic activity; It was initially investigated as an potential antidepressant, however, it is currently under clinical trial for the potential treatment of female sexual dysfunction
References
Certificates
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Extra info
E Jolly et al. Design of Phase III pivotal trials of flibanserin in female Hypoactive Sexual Desire Disorder (HSDD). Sexologies. 2008, 17, Supplement 1, S133-S134.
F Borsini et al. Pharmacology of flibanserin. CNS Drug Rev. 2002, 8 (2), 117–142.
Certificate of Analysis
Material Safety Data Sheet
CNS
5-HT1A
5-HT2A
D4
A19
5-HT1A agonist and 5-HT2A antagonist
Chemical name
1-[2-[4-(3-trifluoromethylphenyl)piperazin-1-yl]ethyl]benzimidazol-[1H]-2-one
Parent CAS No.
[167933-07-5 ]
Order
Size
Unit Price
Stock
10 mg
€95.00
In Stock | | axonmedchem |