| 产品标题 |
产品货号 |
产品规格 |
厂家 |
| E 5555 hydrobromide - Atopaxar hydrobromide | Axon 2030
CAS [474550-69-1]
MF C29H38FN3O5.HBrMW 608.54
Purity:
99%
Soluble in DMSO
Description
Potent and orally active thrombin receptor (or protease-activated receptor 1, PAR1) antagonist (IC50: 19 nM); E5555 showed potent inhibitory effects on human platelet aggregation induced by thrombin and TRAP with IC50 values of 64 and 31nM, respectively
References
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LV Serebruany et al. The in-vitro effects of E5555, a protease-activated receptor (PAR)-1 antagonist, on platelet biomarkers in healthy volunteers and patients with coronary artery disease. Thromb. Haemost. 2009, 102(1), 111-119.
S Goto et al. Double-blind, placebo-controlled Phase II studies of the protease-activated receptor 1 antagonist E5555 (atopaxar) in Japanese patients with acute coronary syndrome or high-risk coronary (...). Eur. Heart J. 2010, 31(21), 2601-2613.
M Kogushi et al. The novel and orally active thrombin receptor antagonist E5555 (Atopaxar) inhibits arterial thrombosis without affecting bleeding time in guinea pigs. Eur. J. Pharmacol. 2011, 657(1-3), 131-137.
Y Kai et al. Prevention of the hypercontractile response to thrombin by proteinase-activated receptor-1 antagonist in subarachnoid hemorrhage. Stroke. 2007 Dec;38(12):3259-65.
Certificate of Analysis
Material Safety Data Sheet
Cardiovascular
Cell Signaling & Oncology
A15
Thrombin (PAR)
Potent and orally active PAR1 antagonist
Chemical name
1-(3-tert-butyl-4-methoxy-5-morpholinophenyl)-2-(5,6-diethoxy-7-fluoro-1-iminoisoindolin-2-yl)ethanone hydrobromide
Parent CAS No.
[751475-53-3]
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Size
Unit Price
Stock
2 mg
€115.00
In Stock | | axonmedchem |
| ML 161 | Axon 1928
CAS [423735-93-7]
MF C17H17BrN2O2MW 361.23
Purity:
98%
Soluble in DMSO and Ethanol
Description
Allosteric inhibitor of protease-activated receptor 1 (PAR1); ML161 inhibits PAR1-mediated platelet activation with nanomolar potentcy
References
Certificates
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Extra info
C Dockendorff et al. Discovery of 1,3-Diaminobenzenes as Selective Inhibitors of Platelet Activation at the PAR1 Receptor. ACS Med Chem Lett. 2012, 3(3), 232-237.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
A15
Thrombin (PAR)
Allosteric inhibitor of PAR1
Chemical name
2-bromo-N-(3-butyramidophenyl)benzamide
Parent CAS No.
[423735-93-7]
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Size
Unit Price
Stock
10 mg
€90.00
In Stock | | axonmedchem |
| SCH 530348 - Vorapaxar | MK 5348 | Axon 1755
CAS [618385-01-6]
MF C29H33FN2O4MW 492.58
Purity:
99%
Optical purity:
Optically pure
Soluble in DMSO
Description
Potent and orally active thrombin receptor (or protease-activated receptor 1, PAR-1) antagonist (Ki value 8.1 nM) that inhibits thrombin-induced platelet activation.
KEYWORDS: SCH 530348 | supplier | PAR1 antagonist | Vorapaxar | MK 5348 | SCH530348 | MK5348 | CAS [618385-01-6] | Thrombin | PAR | GPCR | peptide | antiplatelet | atherothrombosis | protease-activated receptor | cardiovascular | | axonmedchem |
| GB 83 | Axon 1622
CAS [1252806-86-2]
MF C32H44N4O4MW 548.72
Purity:
99%
Optical purity:
Optically pure
Soluble in DMSO
Description
Selective antagonist of human protease activated receptor 2 (PAR2) (IC50: 2 micromolar); reversibly inhibits PAR2 activation by both proteases and other PAR2 agonists
References
Certificates
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Extra info
GD Barry et al. Novel agonist and antagonist for human protease activated receptor 2. J. Med. Chem. 2010, 53, 7428-7440.
List of publications utilizing GB 83 (Axon 1622) purchased from Axon Medchem
Certificate of Analysis
Material Safety Data Sheet
Cardiovascular
Cell Signaling & Oncology
A15
Thrombin (PAR)
PAR2 antagonist
Chemical name
N-((S)-3-cyclohexyl-1-((2S,3S)-1-(2,3-dihydrospiro[indene-1,4'-piperidine]-1'-yl)-3-methyl-1-oxopentan-2-ylamino)-1-oxopropan-2-yl)isoxazole-5-carboxamide
Parent CAS No.
[1252806-86-2]
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Size
Unit Price
Stock
1 mg
€110.00
In Stock | | axonmedchem |
| Timolol maleate | Axon 1518
CAS [26921-17-5]
MF C13H24N4O3S.C4H4O4MW 432.49
Purity:
99%
Optical purity:
>98% ee
Soluble in water and DMSO
Description
A β-adrenergic receptor blocker
References
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Certificate of Analysis
Material Safety Data Sheet
Cardiovascular
CNS
Adrenoceptor β1
A17
β1 adrenergic antagonist
Chemical name
(S)-1-tert-Butylamino-3-(4-morpholin-4-yl-[1,2,5]thiadiazol-3-yloxy)-propan-2-ol maleate
Parent CAS No.
[26839-75-8]
Order
Size
Unit Price
Stock
10 mg
€105.00
In Stock | | axonmedchem |
| PNU 37883 hydrochloride | Axon 1274
CAS [57568-80-6]
MF C21H35N3O.HClMW 381.98
Purity:
99%
Soluble in DMSO and Ethanol
Description
Vascular KATP channel blocker
References
Certificates
Categories
Extra info
Cui et al. Different molecular sites of action for the KATP channel inhibitors, PNU-99963 and PNU-37883A. Br. J. Pharmacol. 2003, 139, 122–128.
Kovalev et al. Molecular analysis of the subtype-selective inhibition of cloned KATP channels by PNU-37883A. Br. J. Pharmacol. 2004, 141, 867.
Certificate of Analysis
Material Safety Data Sheet
Cardiovascular
Cell Signaling & Oncology
CNS
Diabetes & Metabolism
KCNJ11
Kir6.2-SUR1
K+ channel blocker (ATP sensitive, vascular)
Chemical name
N-Adamantan-1-yl-N'-cyclohexyl-morpholine-4-carboxamidine hydrochloride
Parent CAS No.
[122252-09-9]
Order
Size
Unit Price
Stock
10 mg
€85.00
In Stock | | axonmedchem |
| JWH 133 | Axon 1418
CAS [259869-55-1]
MF C22H32OMW 312.49
Purity:
96-99%
Soluble in DMSO and Ethanol
Description
Potent selective CB2 agonist.
KEYWORDS: JWH 133 | supplier | CB2 agonist | JWH133 | JWH-133 | CAS [259869-55-1] | Cannabinoids | CB2 | GPCR | spasticity | tremor | multiple sclerosis | MS | angiogenesis | nociception | | axonmedchem |
| CP 945598 hydrochloride - Otenabant hydrochloride | Axon 2119
CAS [686347-12-6]
MF C25H25Cl2N7O.HClMW 546.88
Purity:
99%
Soluble in DMSO
Description
Hydrochloride formulation of the potent and selective cannabinoid CB1 receptor antagonist CP-945,598 (Otenabant HCl; Ki values 0.7 nM and 0.2 nM in binding and functional assays, respectively) for the management of obesity. CP945598 HCl exhibits a >10000 fold selectivity over CB2, and lacks significant, or meaningful, activity at a large panel of receptors, enzymes, and ion channels. Parent molecule available as well (Axon 2015)
References
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Extra info
J.R. Hadcock et al. In vitro and in vivo pharmacology of CP-945,598, a potent and selective cannabinoid CB(1) receptor antagonist for the management of obesity. Biochem Biophys Res Commun. 2010 Apr 2;394(2):366-71.
L.J. Aronne et al. Efficacy and safety of CP-945,598, a selective cannabinoid CB1 receptor antagonist, on weight loss and maintenance. Obesity (Silver Spring). 2011 Jul;19(7):1404-14.
Certificate of Analysis
Material Safety Data Sheet
Cardiovascular
CNS
Diabetes & Metabolism
Pain & Inflammation
CB1
A13
Pfizer Licensed Products
CB1 antagonist
Chemical name
1-(8-(2-chlorophenyl)-9-(4-chlorophenyl)-9H-purin-6-yl)-4-(ethylamino)piperidine-4-carboxamide hydrochloride
Source information
Pfizer compound; Sold for research purposes under agreement from Pfizer Inc.
Parent CAS No.
[686344-29-6]
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Size
Unit Price
Stock
10 mg
€135.00
In Stock | | axonmedchem |
| CP 945598 - Otenabant | Axon 2015
CAS [686344-29-6]
MF #N/AMW 510.42
Purity:
98%
Soluble in 0.1N HCl(aq) and DMSO
Description
Potent and selective cannabinoid CB1 receptor antagonist (Ki values 0.7 nM and 0.2 nM in binding and functional assays, respectively) for the management of obesity. CP945598 exhibits a >10000 fold selectivity over CB2, and lacks significant, or meaningful, activity at a large panel of receptors, enzymes, and ion channels. Available as HCl salt as well (Axon 2119)
References
Certificates
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Extra info
J.R. Hadcock et al. In vitro and in vivo pharmacology of CP-945,598, a potent and selective cannabinoid CB(1) receptor antagonist for the management of obesity. Biochem Biophys Res Commun. 2010 Apr 2;394(2):366-71.
L.J. Aronne et al. Efficacy and safety of CP-945,598, a selective cannabinoid CB1 receptor antagonist, on weight loss and maintenance. Obesity (Silver Spring). 2011 Jul;19(7):1404-14.
Certificate of Analysis
Material Safety Data Sheet
Cardiovascular
CNS
Diabetes & Metabolism
Pain & Inflammation
CB1
A13
Pfizer Licensed Products
CB1 antagonist
Chemical name
1-(8-(2-chlorophenyl)-9-(4-chlorophenyl)-9H-purin-6-yl)-4-(ethylamino)piperidine-4-carboxamide
Source information
Pfizer compound; Sold for research purposes under agreement from Pfizer Inc.
Parent CAS No.
[686344-29-6]
Order
Size
Unit Price
Stock
10 mg
€135.00
In Stock | | axonmedchem |
| SR 144528 | Axon 1924
CAS [192703-06-3]
MF C29H34ClN3OMW 476.05
Purity:
99%
Soluble in DMSO
Description
Potent and highly selective CB2 receptor antagonist and/or an inverse agonist, with a Ki of 0.6 nM at CB2 and 400 nM at the related CB1 receptor; Useful chemical probe in researching CB2 receptor
References
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Extra info
M Rinaldi-Carmona et al. SR 144528, the first potent and selective antagonist of the CB2 cannabinoid receptor. J. Pharmacol. Exp. Ther. 1998, 284 (2), 644–50.
M Portier et al. SR 144528, an antagonist for the peripheral cannabinoid receptor that behaves as an inverse agonist. J. Pharmacol. Exp. Ther. 1999, 288 (2), 582-589.
Certificate of Analysis
Material Safety Data Sheet
CNS
Pain & Inflammation
CB2
A13
CB2 receptor antagonist and/or an inverse agonist
Chemical name
5-(4-chloro-3-methylphenyl)-1-(4-methylbenzyl)-N-((1S,2S,4R)-1,3,3-trimethylbicyclo[2.2.1]heptan-2-yl)-1H-pyrazole-3-carboxamide
Parent CAS No.
[192703-06-3]
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Size
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Stock
5 mg
€120.00
In Stock | | axonmedchem |
| SLV 319, rac-(±)- | Axon 1712
CAS [362519-49-1]
MF C23H20Cl2N4O2SMW 487.40
Purity:
99%
Soluble in DMSO
Description
Racemate of the potent and highly selective CB1 antagonist Ibipinabant (Axon 1713, Ki value 25 nM and >1000 nM for CB1 and CB2, respectively).
References
Certificates
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Extra info
JH Lange etal. Synthesis, biological properties, and molecular modeling investigations of novel 3,4-diarylpyrazolines as potent and selective CB(1) cannabinoid receptor antagonists. J. Med. Chem. 2004, 47(3), 627–643.
JH Lange and CG Kruse. Recent advances in CB1 cannabinoid receptor antagonists. Curr. Opin. Drug Discov. Devel. 2004, 7(4), 498-506.
AB Need et al. The relationship of in vivo central CB1 receptor occupancy to changes in cortical monoamine release and feeding elicited by CB1 receptor antagonists in rats. Psychopharmacol. 2006, 184(1), 26–35.
JH Lange et al. Design, synthesis, biological properties, and molecular modeling investigations of novel tacrine derivatives with a combination of acetylcholinesterase inhibition and cannabinoid CB1 receptor.... J. Med. Chem. 2010, 53, 1338-1346.
Certificate of Analysis
Material Safety Data Sheet
Cardiovascular
CNS
Diabetes & Metabolism
Pain & Inflammation
CB1
A13
Racemate of CB1 antagonist Ibipinabant (Axon 1713)
Chemical name
3-(4-chlorophenyl)-N'-(4-chlorophenylsulfonyl)-N-methyl-4-phenyl-4,5-dihydro-1H-pyrazole-1-carboximidamide
Parent CAS No.
[362519-49-1]
Order
Size
Unit Price
Stock
5 mg
€110.00
In Stock | | axonmedchem |
| GW 842166X | Axon 1925
CAS [666260-75-9]
MF C18H17Cl2F3N4O2MW 449.25
Purity:
98%
Soluble in DMSO
Description
Potent and selective cannabinoid CB2 receptor agonist; with an oral ED50 of 0.1 mg/kg in the rat FCA model of inflammatory pain; clinical candidate.
KEYWORDS: GW 842166X | supplier | CB2 antagonist | GW842166X | CAS [666260-75-9] | Cannabinoids | CB1 | Agonist | Receptors | | axonmedchem |
| SLV 319, (R)-(+)- - R-SLV319 | Axon 1714
CAS [656827-86-0]
MF C23H20Cl2N4O2SMW 487.40
Purity:
99%
Optical purity:
>98% ee
Soluble in DMSO
Description
Less active (ca 100-fold) enantiomer of SLV 319 (Axon 1713) that is a potent and selective CB1 receptor antagonist
References
Certificates
Categories
Extra info
JH Lange etal. Synthesis, biological properties, and molecular modeling investigations of novel 3,4-diarylpyrazolines as potent and selective CB(1) cannabinoid receptor antagonists. J. Med.l Chem. 2004, 47(3), 627–643.
JH Lange and CG Kruse. Recent advances in CB1 cannabinoid receptor antagonists. Curr. Opin. Drug Discov. Devel. 2004, 7(4), 498-506.
AB Need et al. The relationship of in vivo central CB1 receptor occupancy to changes in cortical monoamine release and feeding elicited by CB1 receptor antagonists in rats. Psychopharmacol. 2006, 184(1), 26–35.
Certificate of Analysis
Material Safety Data Sheet
Cardiovascular
CNS
Diabetes & Metabolism
CB1
A13
Inactive enantiomer of SLV 319
Chemical name
(R)-(+)-3-(4-chlorophenyl)-N'-(4-chlorophenylsulfonyl)-N-methyl-4-phenyl-4,5-dihydro-1H-pyrazole-1-carboximidamide
Parent CAS No.
[656827-86-0]
Order
Size
Unit Price
Stock
2 mg
€95.00
In Stock | | axonmedchem |
| SLV 319 - Ibipinabant | SLV 319, (S)-(-)- | Axon 1713
CAS [464213-10-3]
MF C23H20Cl2N4O2SMW 487.40
Purity:
100%
Optical purity:
>98% ee
Soluble in DMSO
Description
Potent and highly selective CB1 antagonist (Ki= 7.8 and 7943 nM for CB1 and peripheral cannabinoid CB2, respectively); more potent (100-fold) S-(-)-enantiomer in comparison with opposite R(+)-SLV319 (Axon 1714)
References
Certificates
Categories
Extra info
JH Lange etal. Synthesis, biological properties, and molecular modeling investigations of novel 3,4-diarylpyrazolines as potent and selective CB(1) cannabinoid receptor antagonists. J. Med.l Chem. 2004, 47(3), 627–643.
JH Lange and CG Kruse. Recent advances in CB1 cannabinoid receptor antagonists. Curr. Opin. Drug Discov. Devel. 2004, 7(4), 498-506.
AB Need et al. The relationship of in vivo central CB1 receptor occupancy to changes in cortical monoamine release and feeding elicited by CB1 receptor antagonists in rats. Psychopharmacol. 2006, 184(1), 26–35.
Certificate of Analysis
Material Safety Data Sheet
Cardiovascular
CNS
Diabetes & Metabolism
Pain & Inflammation
CB1
A13
CB1 antagonist
Chemical name
(S)-(-)-3-(4-chlorophenyl)-N'-(4-chlorophenylsulfonyl)-N-methyl-4-phenyl-4,5-dihydro-1H-pyrazole-1-carboximidamide
Parent CAS No.
[464213-10-3]
Order
Size
Unit Price
Stock
2 mg
€105.00
In Stock | | axonmedchem |
| PSNCBAM 1 | Axon 1565
CAS [877202-74-9]
MF C22H21ClN4OMW 392.88
Purity:
99%
Soluble in DMSO
Description
An allosteric CB1 receptor antagonist, potentially an anti-obesity agents
References
Certificates
Categories
Extra info
JG Horswill et al. PSNCBAM-1, a novel allosteric antagonist at cannabinoid CB1 receptors with hypophagic effects in rats. Br. J. Pharmacol. 2007, 152(5), 565-6.
JG Horswill et al. Characterisation of PSNCBAM-1, a novel allosteric antagonist of the cannabinoid type 1 receptor with in vivo efficacy in an acute rat feeding model. PBPS 2006.
Certificate of Analysis
Material Safety Data Sheet
Diabetes & Metabolism
Miscellaneous
Pain & Inflammation
CB1
A13
CB1 antagonist (allosteric)
Chemical name
1-(4-Chloro-phenyl)-3-[3-(6-pyrrolidin-1-yl-pyridin-2-yl)-phenyl]-urea
Parent CAS No.
[877202-74-9]
Order
Size
Unit Price
Stock
5 mg
€80.00
In Stock | | axonmedchem |
| Iodopravadoline - AM 630 | Axon 1574
CAS [164178-33-0]
MF C23H25IN2O3MW 504.36
Purity:
99%
Soluble in DMSO
Description
Selective cannabinoid (CB) receptor antagonist.
KEYWORDS: Iodopravadoline | supplier | CB2 antagonist | AM 630 | AM630 | CAS [164178-33-0] | Cannabinoid | CB2 | Antagonist | competitive | protean | inverse agonist | intrinsic activity | | axonmedchem |
| MK 0364 - Taranabant | Axon 1550
CAS [701977-09-5]
MF C27H25ClF3N3O2MW 515.95
Purity:
98%
Optical purity:
Optically pure
Soluble in DMSO
Description
Potent and selective cannabinoid receptor type 1 (CB1) antagonist and/or inverse agonist
References
Certificates
Categories
Extra info
TM Fong et al. Antiobesity efficacy of a novel cannabinoid-1 receptor inverse agonist, MK-0364, in rodents. J. Pharmacol. Exp. Ther. 2007, 321(3), 1013-1022.
MS Kipnes et al. A one-year study to assess the safety and efficacy of the CB1R inverse agonist taranabant in overweight and obese patients with type 2 diabetes. Diabetes, Obesity & Metabolism 2010, 12 (6), 517–31.
Certificate of Analysis
Material Safety Data Sheet
Cardiovascular
CNS
Diabetes & Metabolism
Pain & Inflammation
CB1
A13
CB1 antagonist/inverse agonist
Chemical name
N-[(1S,2S)-3-(4-Chloro-phenyl)-2-(3-cyano-phenyl)-1-methyl-propyl]-2-methyl-2-(5-trifluoromethyl-pyridin-2-yloxy)-propionamide
Parent CAS No.
[701977-09-5]
Order
Size
Unit Price
Stock
2 mg
€95.00
In Stock | | axonmedchem |
| HU 308 | Axon 1440
CAS [256934-39-1]
MF C27H42O3MW 414.62
Purity:
98%
Soluble in DMSO
Description
Potent cannabinoid agonist specific at CB2 (Ki values >10 µM and 22.7 nM for CB1 and CB2, respectively). It has analgesic effects, promotes proliferation of neural stem cells, and protects both liver and blood vessel tissues against oxidative stress via inhibition of TNF-α.
KEYWORDS: HU 308 | supplier | CB2 agonist | HU308 | CAS [256934-39-1] | Cannabinoids | CB2 | GPCR | CNS | blood pressure | hypertension | inflammation | pain | defecation | anti-inflammatory | analgesic | | axonmedchem |
| SR 141716 hydrochloride - Rimonabant hydrochloride | Axon 1220
CAS [158681-13-1]
MF C22H21Cl3N4O.HClMW 500.25
Purity:
99%
Soluble in DMSO and Ethanol
Description
Selective, potent and orally active antagonist of the cannabinoid CB1 receptor with a long duration of action (Ki value 2 nM).
KEYWORDS: SR 141716 hydrochloride | supplier | CB1 antagonist | Rimonabant hydrochloride | supplier | SR141716 | CAS [158681-13-1] | [168273-06-1] | Cannabinoids | CB1 | Antagonist | metabolism | gastrointestinal motility | obesity | food intake | | axonmedchem |
| AM 281 | Axon 1219
CAS [202463-68-1]
MF C21H19Cl2IN4O2MW 557.21
Purity:
99%
Soluble in DMSO
Description
Potent and selective CB1 cannabinoid receptor antagonist/inverse agonist
References
Certificates
Categories
Extra info
F Molina-Holgado et al. Neuroprotective effects of the synthetic cannabinoid HU-210 in primary cortical neurons are mediated by phosphatidylinositol 3-kinase/AKT signaling. Mol. Cell. Neurosci. 2005, 28, 189-194.
AN Gifford et al. Effect of the cannabinoid receptor SPECT agent, AM 281, on hippocampal acetylcholine release from rat brain slices. Neurosci. Lett. 1997, 238, 84-86.
Certificate of Analysis
Material Safety Data Sheet
Cardiovascular
CNS
Diabetes & Metabolism
Pain & Inflammation
CB1
A13
CB1 antagonist
Chemical name
1-(2,4-Dichloro-phenyl)-5-(4-iodo-phenyl)-4-methyl-1H-pyrazole-3-carboxylic acid morpholin-4-ylamide
Parent CAS No.
[202463-68-1]
Order
Size
Unit Price
Stock
10 mg
€95.00
In Stock | | axonmedchem |
| Flupirtine maleate - D 9998 | Katadolon | Axon 1437
CAS [75507-68-5]
MF C15H17FN4O2.C4H4O4MW 420.39
Purity:
99%
Soluble in DMSO
Description
A centrally acting, nonopioid analgesic; flupirtine has a functional profile similar to NMDA-receptor antagonists, but devoid of the typical side effects of these drugs; flupirtine exerts potent cyto- and neuroprotective actions in different in vivo and in vitro models
References
Certificates
Categories
Extra info
MD Swedberg et al. Pharmacological mechanisms of action of flupirtine: a novel, centrally acting, nonopioid analgesic evaluated by its discriminative effects in the rat. J. Pharmacol. Exp. Ther. 1998, 246(3), 1067–74.
S Dhar et al. Flupirtine blocks apoptosis in batten patient lymphoblasts and in human postmitotic CLN3- and CLN2-deficient neurons. Ann. Neurol. 2002, 51 (4), 448–66.
G. Schuster et al. Flupirtine: A Review of Its Neuroprotective and Behavioral Properties. CNS Drug Reviews, 1998, 4(2), 149-164.
Certificate of Analysis
Material Safety Data Sheet
Cardiovascular
CNS
Pain & Inflammation
Kv7.1
KCNQ1
Analgesic
Chemical name
[2-Amino-6-(4-fluoro-benzylamino)-pyridin-3-yl]-carbamic acid ethyl ester maleate
Parent CAS No.
[56995-20-1]
Order
Size
Unit Price
Stock
10 mg
€65.00
In Stock | | axonmedchem |
| Hydroxychloroquine sulfate - NSC 4375 | Axon 2432
CAS [747-36-4]
MF C18H26ClN3O.H2SO4MW 433.95
Purity:
99%
Optical purity:
Racemate
Soluble in water
Description
Antimalarial drug (HCQ) and immunosuppressive lysosomotropic amine, also used as a slow-acting anti-rheumatic drug and for treatment of lupus erythematosus. HCQ is also shown to act as an antagonist for Toll-like receptors (TLR-7 and TLR-9) in plasmacytoid dendritic cells (pDCs).
KEYWORDS: Hydroxychloroquine sulfate | supplier | Antimalarial drug | NSC 4375 | NSC4375 | CAS [747-36-4] | [118-42-3] | HCQ | malaria | beta-hematin | Plasmodium | hemoglobin | hemozoin | TLR | toll-like receptor | lupus erythematosus | SLE | TLR-9 | TLR-7 | | axonmedchem |
| AM 251 | Axon 1218
CAS [183232-66-8]
MF C22H21Cl2IN4OMW 555.24
Purity:
99%
Soluble in DMSO and Ethanol
Description
Cannabinoids CB1 antagonist, structurally very close to SR 141716A (rimonabant). AM251: Ki 7.5 nM for CB1 receptor vs SR 141716A ( Ki value of 11.5 nM). However AM251 is about two-fold more selective for the CB1 receptor when compared to SR 141716A
References
Certificates
Categories
Extra info
R Lan et al. Structure-activity relationships of pyrazole derivatives as cannabinoid receptor antagonists. J. Med. Chem. 1999, 42 769-776.
Certificate of Analysis
Material Safety Data Sheet
Cardiovascular
CNS
Diabetes & Metabolism
Pain & Inflammation
CB1
A13
CB1 antagonist
Chemical name
1-(2,4-Dichloro-phenyl)-5-(4-iodo-phenyl)-4-methyl-1H-pyrazole-3-carboxylic acid piperidin-1-ylamide
Parent CAS No.
[183232-66-8]
Order
Size
Unit Price
Stock
10 mg
€95.00
In Stock | | axonmedchem |
| KRP 203 | Axon 1615
CAS [509088-69-1]
MF C24H26ClNO3S.HClMW 480.45
Purity:
98%
Soluble in DMSO
Description
Selective sphingosine-1-phosphate (S1P) receptor 1 agonist; immunosuppressant.
Note: | | axonmedchem |
| Vidofludimus - 4SC-101 | SC 12267 | Axon 2377
CAS [717824-30-1]
MF C20H18FNO4MW 355.36
Purity:
99%
Soluble in DMSO
Description
Oral immunomodulatory drug that inhibits dihydroorotate dehydrogenase (DHODH; IC50 value 134 nM for human DHODH mediated DCIP reduction) and lymphocyte proliferation in vitro. Vidofludimus inhibits the proliferation of human peripheral blood mononuclear cells (PBMCs) stimulated with Phytohemagglutinin-L, and interleukin (IL)-17 secretion from human peripheral blood mononuclear cells in a dose-related fashion (IC50 of 6 µM approx.) and independently of lymphocyte proliferation. May be applied for treatment of rheumatoid arthritis and inflammatory bowel disease, and as immunosuppressant after renal transplantation.
References
Certificates
Categories
Extra info
J. Leban et al. SAR, species specificity, and cellular activity of cyclopentene dicarboxylic acid amides as DHODH inhibitors. Bioorg. Med. Chem. Lett. 2005, 15, 4854-4857.
K. Rusai et al. Immunosuppression with 4SC-101, a novel inhibitor of dihydroorotate dehydrogenase, in a rat model of renal transplantation. Transplantation. 2012, 93, 1101-1107.
L.R. Fitzpatrick et al. Vidofludimus inhibits colonic interleukin-17 and improves hapten-induced colitis in rats by a unique dual mode of action. J. Pharmacol. Exp. Ther. 2012, 342, 850-860.
L.R. Fitzpatrick et al. Inhibition of IL-17 as a pharmacological approach for IBD. Int. Rev. Immunol. 2013, 32, 544-555.
Certificate of Analysis
Material Safety Data Sheet
Immunology
Pain & Inflammation
Immunomodulator
DHODH
EC 1.3.3.1
Oral immunomodulatory drug that inhibits dihydroorotate dehydrogenase (DHODH)
Chemical name
2-(3-fluoro-3'-methoxybiphenyl-4-ylcarbamoyl)cyclopent-1-enecarboxylic acid
Parent CAS No.
[717824-30-1]
Order
Size
Unit Price
Stock
5 mg
€125.00
In Stock | | axonmedchem |
| Chloroquine diphosphate - NSC 14050 | Axon 2431
CAS [50-63-5]
MF C18H26ClN3.2H3PO4MW 515.86
Purity:
99%
Optical purity:
Racemate
Soluble in water
Description
Classical antimalarial drug (CQ) with lysosomotropic effects causing necrosis and apoptosis. Inhibitor of hemozoin (β-hematin) formation in malaria (Plasmodium strains) affected red blood cells. Nowadays, most of the Plasmodium falciparum strains are resistant to this drug. Chloroquine was found to inhibit the human thiamine transporter ThTr-2 (SLC19A3), and to inhibit cell growth and to induce cell death in A549 lung cancer cells.
KEYWORDS: Chloroquine diphosphate | supplier | Antimalarial drug | NSC 14050 | NSC14050 | CQ | CAS [50-63-5] | [54-05-7] | beta-hematin | Plasmodium | hemoglobin | hemozoin | thiamine | transporter | ThTr-2 | SLC19A3 | apoptosis | necrosis | | axonmedchem |
| Tacrolimus - FK 506 | Axon 2263
CAS [104987-11-3]
MF C44H69NO12MW 804.02
Purity:
99%
Optical purity:
Optically pure
Soluble in DMSO
Description
Potent Calcineurin inhibitor (calcium dependent serine/threonine protein phosphatase 2B). The mechanism of action of FK 506 (Tacrolimus) involves the formation of a molecular complex with the the immunophilin FKBP12 (IC50 value 3 nM), to reduce its peptidyl-prolyl isomerase activity. Tacrolimus potently inhibits T-cell activation-induced TNF-α, IL-1β, IL-2, IL-3, IL-4, and IL-6 production, but does not affect LPS-induced cytokine production and proliferation of normal cells, such as bone marrow cells.
Immunosuppressant, neuroprotectant and anticonvulsant.
References
Certificates
Categories
Extra info
A.W. Thomson et al. Mode of action of tacrolimus (FK506): molecular and cellular mechanisms. Ther. Drug Monit. 1995, 17, 584-591.
G. Sierra-Paredes et al. Ascomycin and FK506: pharmacology and therapeutic potential as anticonvulsants and neuroprotectants. CNS Neurosci. Ther. 2008, 14, 36-46.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Signaling & Oncology
Epigenetics
Immunology
Pain & Inflammation
Immunomodulator
NF-κB
MAPK
Calcineurin
EC 3.1.3.16
Potent Calcineurin (Ca2+ dependent protein phosphatase 2B) inhibitor
Chemical name
(3S,4R,5S,8R,9E,12S,14S,15R,16S,18R,19R,26aS)-5,6,8,11,12,13,14,15,16,17,18,19,24,25,26,26a-Hexadecahydro-5,19-dihydroxy-3-[(1E)-2-[(1R,3R,4R)-4-hydroxy-3-methoxycyclohexyl]-1-methylethenyl]-14,16-dimethoxy-4,10,12,18-tetramethyl-8-(2-propen-1-yl)-15,19-e
Parent CAS No.
[104987-11-3]
Order
Size
Unit Price
Stock
10 mg
€100.00
In Stock | | axonmedchem |
| Avridine - CP 20961 | Axon 2099
CAS [35607-20-6]
MF C43H90N2O2MW 667.19
Purity:
99%
Soluble in DMSO and Ethanol
Description
A lipoidal amine with interferon-inducing and adjuvant properties; an effective adjuvant for Newcastle disease antigen (NDA) in chickens; a potent adjuvant that can induce arthritis in most rat strains; immunomodulator
References
Certificates
Categories
Extra info
NF Pierce & JB Sacci. Enhanced mucosal priming by cholera toxin and procholeragenoid with a lipoidal amine adjuvant (avridine) delivered in liposomes. Infection and immunity, 1984, 44(2), 469-473.
MM Rweyemamu et al. Efficacy of avridine as an adjuvant for Newcastle disease virus antigen in chickens. Am. J. Veterinary Res. 1986, 47(6), 1243-1248.
Certificate of Analysis
Material Safety Data Sheet
Immunology
Pain & Inflammation
Immunomodulator
IFN
Pfizer Licensed Products
Lipoidal amine; interferon-inducing and adjuvant properties
Chemical name
2,2'-(3-(dioctadecylamino)propylazanediyl)diethanol
Source information
Pfizer compound; Sold for research purposes under agreement from Pfizer Inc.
Parent CAS No.
[35607-20-6]
Order
Size
Unit Price
Stock
10 mg
€80.00
In Stock | | axonmedchem |
| Tofacitinib citrate - CP 690550-10 | Axon 2072
CAS [540737-29-9]
MF C16H20N6O.C6H8O7MW 504.49
Purity:
99%
Soluble in DMSO
Description
Potent Janus Kinase 3 (JAK3) inhibitor; an immunosuppressive agent exhibiting potent effects in preclinical transplantation and arthritis models; clinically safe and effective in preventing transplant rejection and improving symptoms of rheumatoid arthritis and psoriasis; the citrate salt form of CP 690550 - Tofacitinib (Axon 1338)
References
Certificates
Categories
Extra info
AC Papageorgiou et al. Is JAK3 a new drug target for immunomodulation-based therapies? Trends Pharmacol. Sci. 2004, 25(11), 558-562.
E Kudlacz et al. The novel JAK-3 inhibitor CP-690550 is a potent immunosuppressive agent in various murine models. Am. J. Transplant. 2004, 4, 51-57.
E Kudlacz et al. The JAK-3 inhibitor CP-690550 is a potent anti-inflammatory agent in a murine model of pulmonary eosinophilia. Eur. J. Pharmacol. 2008, 582, 154-161.
PS Changelian et al. Prevention of Organ Allograft Rejection by a Specific Janus Kinase 3 Inhibitor. Sci. 2003, 302(5646), 875-878.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Epigenetics
Immunology
Pain & Inflammation
Immunomodulator
JAK-STAT
EC 2.7.10.2
JAK
Pfizer Licensed Products
Potent Janus Kinase 3 (JAK3) inhibitor
Chemical name
3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)-3-oxopropanenitrile 2-hydroxypropane-1,2,3-tricarboxylate
Source information
Pfizer compound; Sold for research purposes under agreement from Pfizer Inc.
Parent CAS No.
[477600-75-2]
Order
Size
Unit Price
Stock
10 mg
€115.00
In Stock | | axonmedchem |
| Laquinimod - ABR 215062 | Axon 1970
CAS [248281-84-7]
MF C19H17ClN2O3MW 356.80
Purity:
99%
Soluble in DMSO
Description
A selective autoimmune suppressant investigated as an oral treatment for multiple sclerosis (MS) and other autoimmune diseases; Immunomodulator
References
Certificates
Categories
Extra info
G Comi et al. Effect of laquinimod on MRI-monitored disease activity in patients with relapsing-remitting multiple sclerosis: a multicentre, randomised, double-blind, placebo-controlled phase IIb study. Lancet 2008, 371(9630), 2085-2092.
JS Yang et al. Laquinimod (ABR-215062) suppresses the development of experimental autoimmune encephalomyelitis, modulates the Th1/Th2 balance and induces the Th3 cytokine TGF-β in Lewis rats. J. Neuroimmunol. 2004, 156(1–2), 3–9.
Certificate of Analysis
Material Safety Data Sheet
Immunology
Miscellaneous
Immunomodulator
Selective autoimmune suppressant; Immunomodulator
Chemical name
5-chloro-N-ethyl-4-hydroxy-1-methyl-2-oxo-N-phenyl-1,2-dihydroquinoline-3-carboxamide
Parent CAS No.
[248281-84-7]
Order
Size
Unit Price
Stock
10 mg
€95.00
In Stock | | axonmedchem |
| AMD 3100 - Plerixafor | SID 791 | JM 3100 | Axon 1738
CAS [155148-31-5]
MF C28H54N8.8HClMW 794.47
Purity:
100%
Soluble in water
Description
Highly potent and selective chemokine CXCR4 receptor antagonist, with IC50 values to be 0.02-0.13 and >25 μM for CXCR4 and all other chemokine receptors respectively); HIV inhibitor; an immunostimulant used to multiply hematopoietic stem cells in cancer patients
References
Certificates
Categories
Extra info
E De Clercq et al. Highly potent and selective inhibition of human immunodeficiency virus by the bicyclam derivative JM3100. Antimicrob. agents chemother. 1994, 38(4), 668–74.
SL Davies et al. Plerixafor Hydrochloride. Drugs Fut. 2007, 32(2), 123.
AF Cashen et al. AMD3100: CXCR4 antagonist and rapid stem cell-mobilizing agent. Future Oncol. 2007, 3(1), 19–27.
G Calandra et al. AMD3100 plus G-CSF can successfully mobilize CD34+ cells from non-Hodgkin's lymphoma, Hodgkin's disease and multiple myeloma patients previously failing mobilization with chemotherapy (...). Bone Marrow Transpl. 2008, 41, 331–338.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Immunology
Stem Cell
Immunomodulator
A2
Chemokine
CXCR4 antagonist
Chemical name
1,4-bis((1,4,8,11-tetraazacyclotetradecan-1-yl)methyl)benzene octahydrochloride
Parent CAS No.
[110078-46-1]
Order
Size
Unit Price
Stock
10 mg
€85.00
In Stock | | axonmedchem |
| Lenalidomide - CC 5013 | Revimid | Axon 1793
CAS [191732-72-6]
MF C13H13N3O3MW 259.26
Purity:
100%
Soluble in DMSO
Description
Anti-angiogenesis agent; immunomodulator; a FDA approved drug to treat mantle cell lymphoma, multiple myeloma, and anemia caused by a certain type of myelodysplastic syndrome (MDS). It is being studied in the treatment of other conditions and types of cancer. Lenalidomide may help the immune system kill abnormal blood cells or cancer cells. It may also prevent the growth of new blood vessels that tumors need to grow
References
Certificates
Categories
Extra info
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Signaling & Oncology
Immunology
Pain & Inflammation
Immunomodulator
TNF-R1 (CD120)
NF-κB
Type 1
TNFα inhibitor. Immunomodulator.
Chemical name
3-(4-amino-1-oxoisoindolin-2-yl)piperidine-2,6-dione
Parent CAS No.
[191732-72-6]
Order
Size
Unit Price
Stock
10 mg
€75.00
In Stock | | axonmedchem |
| Sotrastaurin - AEB 071 | NVP-AEB 071 | Axon 1635
CAS [425637-18-9]
MF C25H22N6O2MW 438.48
Purity:
99%
Soluble in 0.1N HCl(aq) and DMSO
Description
Potent and specific inhibitor of protein kinase C (PKC) with Ki at subnanomolar to low nanomolar range for a variety of PKC isotypes while selective for >200 other kinases; an immunosuppressant that blocks early T-lymphocyte (T-cell) activation via protein kinase C inhibition.
KEYWORDS: Sotrastaurin | supplier | PKC inhibitor | AEB 071 | NVP-AEB071 | Sotrastaurin | AEB071 | NVP-AEB 071 | AEB-071 | CAS [425637-18-9] | Non Selective (Phosphorylation Substrates) | PKC | Inhibitor | Enzymes | | axonmedchem |
| STF 083010 | Axon 1670
CAS [307543-71-1]
MF C15H11NO3S2MW 317.38
Purity:
99%
Soluble in DMSO
Description
Specific IRE1α endonuclease inhibitor without affecting its kinase activity; shows significant antimyeloma activity in human MM xenografts
References
Certificates
Categories
Extra info
I Papandreou et al. Identification of an Ire1alpha endonuclease specific inhibitor with cytotoxic activity against human multiple myeloma. Blood 2011, 117, 1311-1314.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Signaling & Oncology
Immunomodulator
EC 2.7.11.1
IRE
Endonuclease
IRE1α inhibitor
Chemical name
(E/Z)-N-((2-hydroxynaphthalen-1-yl)methylene)thiophene-2-sulfonamide
Parent CAS No.
[307543-71-1]
Order
Size
Unit Price
Stock
10 mg
€95.00
In Stock | | axonmedchem |
| MNITMT - NSC 631156 | Axon 1267
CAS [177653-76-8]
MF C7H8N6O2SMW 240.24
Purity:
99%
Soluble in Ethanol
Description
Immunosuppressant
References
Certificates
Categories
Extra info
H Tumah et al. Biochemical, Cytotoxic and Genotoxic Effects of a Novel Non-Mercaptopurine Immunosuppressant. Acta Pharmaceutica Sciencia. 2006, 48, 109-119.
http://www.researchgate.net/publication/242586870_Biochemical_Cytotoxic_and_Genotoxic_Effects_of_a_Novel_Non_Mercaptopurine_Immunosuppressant
Certificate of Analysis
Material Safety Data Sheet
Immunology
Miscellaneous
Immunomodulator
Immunosuppressant
Chemical name
4-Methyl-3-(3-methyl-5-nitro-3H-imidazol-4-ylsulfanyl)-4H-[1,2,4]triazole
Parent CAS No.
[177653-76-8]
Order
Size
Unit Price
Stock
10 mg
€75.00
In Stock | | axonmedchem |
| CP 690550 - Tasocitinib | Tofacitinib | Axon 1338
CAS [477600-75-2]
MF C16H20N6OMW 312.37
Purity:
99%
Soluble in 0.1N HCl(aq) and DMSO
Description
Janus Kinase 3 (JAK3) inhibitor; an immunosuppressive agent exhibiting potent effects in preclinical transplantation and arthritis models; clinically safe and effective in preventing transplant rejection and improving symptoms of rheumatoid arthritis and psoriasis.This product is also available as its citrate salt form, Tofacitinib citrate (Axon 2072).
KEYWORDS: CP 690550 | supplier | JAK3 inhibitor | Tasocitinib | Tofacitinib | CP690550 | CP-690550 | CAS [477600-75-2] | JAK-STAT Pathway | JAK | Janus Kinase | immunosuppressive | transplantation | rheumatoid | arthritis | rejection | psoriasis | | axonmedchem |
| CNV 1014802 hydrochloride - GSK 1014802 HCl | GSK2 HCl | Raxatrigine HCl | BIIB 074 HCl | Vixotrigine HCl | Axon 2548
CAS [934240-31-0]
MF C18H19FN2O2.HClMW 350.82
Purity:
99%
Soluble in water and DMSO
Description
Sodium channel blocker with potent anticonvulsant activity; potential for novel treatment for Schizophrenia. CNV 1014802 (GSK2) was tested in clinical trials for treatment of trigeminal neuralgia, and shows selectivity for the Nav1.7 subtype over the other subtypes tested (Nav1.1, Nav1.2, Nav1.3, Nav1.5, Nav1.6 and TTX-R), for both the resting and depolarized states.
The parent molecule of CNV 1014802 (Axon 1899) is available as well.
KEYWORDS: CNV 1014802 hydrochloride | supplier | Na+ channel blocker | GSK 1014802 HCl | GSK2 HCl | Raxatrigine HCl | BIIB 074 HCl | Vixotrigine HCl | CNV1014802 hydrochloride | CNV-1014802 hydrochloride | GSK1014802 HCl | GSK-1014802 HCl | GSK 2 HCl | GSK-2 HCl | BIIB074 HCl | BIIB-074 HCl | CAS [934240-31-0] | [934240-30-9] | Sodium | Nav1.7 | Nav1.2 | Nav1.6 | Nav1.3 | Blocker | Ion Channels | anticonvulsant | Schizophrenia | trigeminal neuralgia | neuropathic | pain | | axonmedchem |
| CNV 1014802 - GSK 1014802 | GSK2 | Raxatrigine | BIIB 074 | Vixotrigine | Axon 1899
CAS [934240-30-9]
MF C18H19FN2O2MW 314.35
Purity:
99%
Optical purity:
Optically pure
Soluble in 0.1N HCl(aq) and DMSO
Description
Sodium channel blocker with potent anticonvulsant activity; potential for novel treatment for Schizophrenia. CNV 1014802 (GSK 1014802 or GSK2 or Raxatrigine) was tested in clinical trials for treatment of trigeminal neuralgia, and shows selectivity for the Nav1.7 subtype over the other subtypes tested (Nav1.1, Nav1.2, Nav1.3, Nav1.5, Nav1.6 and TTX-R), for both the resting and depolarized states.
The water soluble HCl salt of CNV 1014802 (Axon 2548) is available as well
KEYWORDS: CNV 1014802 | supplier | Na+ channel blocker | GSK 1014802 | GSK2 | Raxatrigine | BIIB 074 | Vixotrigine | CNV1014802 | CNV-1014802 | GSK1014802 | GSK-1014802 | GSK 2 | GSK-2 | BIIB074 | BIIB-074 | CAS [934240-30-9] | Sodium | Nav1.7 | Nav1.2 | Nav1.6 | Nav1.3 | Blocker | Ion Channels | anticonvulsant | Schizophrenia | trigeminal neuralgia | neuropathic | pain | | axonmedchem |
| RGH 896 - Radiprodil | Axon 1434
CAS [496054-87-6]
MF C21H20FN3O4MW 397.40
Purity:
99%
Soluble in DMSO
Description
Orally active and selective NMDA NR2B antagonist; a potential therapeutic agent in treatment of neuropathic pain and possibly other chronic pain conditions. It blocks pain signaling without interacting with other NMDA receptor subtypes thus potentially improving therapeutic index and side effect profile
References
Certificates
Categories
Extra info
L Mony et al. Allosteric modulators of NR2B-containing NMDA receptors: molecular mechanisms and therapeutic potential. Br. J. Pharmacol. 2009, 157(8), 1301–1317.
Certificate of Analysis
Material Safety Data Sheet
CNS
Pain & Inflammation
NMDA
Unclassified
NMDA NR2B antagonist
Chemical name
2-[4-(4-Fluoro-benzyl)-piperidin-1-yl]-2-oxo-N-(2-oxo-2,3-dihydro-benzooxazol-6-yl)-acetamide
Parent CAS No.
[496054-87-6]
Order
Size
Unit Price
Stock
5 mg
€95.00
In Stock | | axonmedchem |
| XEN 907 | Axon 2056
CAS [912656-34-9]
MF C21H21NO4MW 351.40
Purity:
99%
Soluble in DMSO
Description
Sodium channel blocker, potent and selective at voltage-gated Nav1.7 (SCN9A)
References
Certificates
Categories
Extra info
S Chowdhury et al. Discovery of XEN907, a spirooxindole blocker of NaV1.7 for the treatment of pain. Bioorg. Med. Chem Lett. 2011, 21(12), 3676-3681.
Certificate of Analysis
Material Safety Data Sheet
CNS
Pain & Inflammation
Nav1.7
Unclassified
Sodium channel blocker (voltage-gated Nav1.7)
Chemical name
1'-pentyl-6H-spiro[benzofuro[6,5-d][1,3]dioxole-7,3'-indolin]-2'-one
Parent CAS No.
[912656-34-9]
Order
Size
Unit Price
Stock
5 mg
€135.00
In Stock | | axonmedchem |
| Nav1.7 blocker 24 - Compound 24 | Axon 1791
CAS [1315451-25-2]
MF C20H16Cl2F3N3O3MW 474.26
Purity:
99%
Soluble in DMSO
Description
Sodium channel blocker, potent and selective at voltage-gated Nav1.7 (SCN9A); with Nav1.7 pIC50 6.75 and Nav1.5 pIC50 <4.48
References
Certificates
Categories
Extra info
I Macsari et al. Phenyl isoxazole voltage-gated sodium channel blockers: structure and activity relationship. Bioorg. Med. Chem. Lett. 2011, 21(13), 3871-3876.
Certificate of Analysis
Material Safety Data Sheet
CNS
Pain & Inflammation
Nav1.7
Unclassified
Nav1.7 blocker
Chemical name
2-(3-(2,6-dichlorophenyl)-5-methylisoxazol-4-yl)-N-((6-(2,2,2-trifluoroethoxy)pyridin-3-yl)methyl)acetamide
Parent CAS No.
[1315451-25-2]
Order
Size
Unit Price
Stock
10 mg
€125.00
In Stock | | axonmedchem |
| A 803467 | Axon 1915
CAS [944261-79-4]
MF C19H16ClNO4MW 357.79
Purity:
98%
Soluble in DMSO
Description
Sodium channel blocker, potent and selective at voltage-gated Nav1.8 channel (IC50: 8 nM).
KEYWORDS: A 803467 | supplier | Nav1.8 blocker | A803467 | A-803467 | CAS [944261-79-4] | Sodium | Nav1.8 | Blocker | Ion Channels | | axonmedchem |
| Lacosamide - SPM 927 | Erlosamide | Axon 1444
CAS [175481-36-4]
MF C13H18N2O3MW 250.29
Purity:
99%
Optical purity:
>98% ee
Soluble in water and DMSO
Description
Lacosamide acts by enhancing slow inactivation of voltage gated sodium channels; a medication for the adjunctive treatment of partial-onset seizures and diabetic neuropathic pain
References
Certificates
Categories
Extra info
AC Errington et al. The investigational anticonvulsant lacosamide selectively enhances slow inactivation of voltage-gated sodium channels. Molecular pharmacology 2008, 73 (1), 157–69.
AC Errington et al. Seeking a mechanism of action for the novel anticonvulsant lacosamide. Neuropharmacology 2006, 50 (8), 1016–1029.
E Ben-Menachem et al. Efficacy and safety of oral lacosamide as adjunctive therapy in adults with partial-onset seizures. Epilepsia 2007, 48 (7), 1308–1317.
RL Rauck et al. Lacosamide in painful diabetic peripheral neuropathy: a phase 2 double-blind placebo-controlled study. Clin J Pain 2007, 23 (2), 150–158.
PL Sheets et al. Differential block of sensory neuronal voltage-gated sodium channels by lacosamide [(2R)-2-(acetylamino)-N-benzyl-3-methoxypropanamide], lidocaine, and carbamazepine. J Pharmacol Exp Ther. 2008 Jul;326(1):89-99.
Certificate of Analysis
Material Safety Data Sheet
CNS
Diabetes & Metabolism
Pain & Inflammation
Nav1.7
Nav1.8
Unclassified
Nav1.3
Na+ channel blocker; anti-convulsant
Chemical name
(R)-2-Acetylamino-N-benzyl-3-methoxy-propionamide
Parent CAS No.
[175481-36-4]
Order
Size
Unit Price
Stock
10 mg
€75.00
In Stock | | axonmedchem |
| AM 36 dihydrochloride - CNSB002 | Axon 1113
CAS [199467-52-2]
MF C27H39ClN2O2.2HClMW 531.99
Purity:
98%
Moderately soluble in water
Description
Na+ channel blocker; neuroprotective agent.
KEYWORDS: AM 36 dihydrochloride | supplier | Na+ channel Blocker | CNSB002 | AM36 |CAS[199467-52-2] | Sodium | Blocker | Ion Channels | Nav1.3 | Nav1.7 | Nav1.8 | neuropathic pain | analgesic | neuroprotective |ROS | | axonmedchem |
| MLN 9708 - Ixazomib citrate | Axon 2557
CAS [1201902-80-8]
MF C20H23BCl2N2O9MW 517.12
Purity:
99%
Soluble in DMSO
Description
Citrate prodrug of MLN 2238 (Ixazomib; Axon 2556), a selective and reversible inhibitor of the β5 subunit sites of the 20S proteasome with antitumor activity in various malignancies. MLN 9708 exhibits improved pharmacodynamics and antitumor activity compared with bortezomib in various B-cell lymphoma models, due to a greater tumor to blood ratio of proteasome inhibition that ultimately translates into improved tumor pharmacodynamic response and antitumor activity in several tumor xenograft models. Approved by the FDA in November 2015 for multiple myeloma treatment.
KEYWORDS: MLN 9708 | supplier | Proteasome inhibitor | Ixazomib citrate | MLN9708 | CAS [1201902-80-8] | Ubiquitin | Proteasome 20S | Inhibitor | MLN2238 | MLN 2238 | prodrug | β5 subunit | B-cell lymphoma | FDA approved | | axonmedchem |
| Nav1.7 blocker 52 - Compound 52 | Axon 1780
CAS [1211866-85-1]
MF C25H27F3N6O3MW 516.52
Purity:
99%
Soluble in DMSO
Description
Potent and state-dependent sodium channel blocker, selective at voltage-gated Nav1.7 (SCN9A); Selectivity over many ion channels and GPCRs, including some selectivity within the sodium channel family
References
Certificates
Categories
Extra info
H Bregman et al. Identification of a potent, state-dependent inhibitor of Nav1.7 with oral efficacy in the formalin model of persistent pain. J. Med. Chem. 2011, 54(13), 4427-4445.
Certificate of Analysis
Material Safety Data Sheet
CNS
Pain & Inflammation
Nav1.7
Unclassified
Nav1.7 blocker
Chemical name
N-(2-methyl-3-(4-(4-(4-(trifluoromethoxy)benzyloxy)piperidin-1-yl)-1,3,5-triazin-2-ylamino)phenyl)acetamide
Parent CAS No.
[1211866-85-1]
Order
Size
Unit Price
Stock
10 mg
€125.00
In Stock | | axonmedchem |
| Salermide | Axon 2704
CAS [1105698-15-4]
MF C26H22N2O2MW 394.47
Purity:
99%
Soluble in DMSO
Description
Salermide is a reverse amide with a potent in vitro inhibitory effect on Sirt1 and Sirt2. Salermide was well tolerated by mice at concentrations up to 100 μM and prompted tumour-specific cell death in a wide range of human cancer cell lines. It induces massive apoptosis in cancer but not in non-transformed cultured cells. The apoptotic effect of Salermide is in part because of the reactivation of proapoptotic genes that are epigenetically repressed by Sirt1 exclusively in cancer cells.
KEYWORDS: Salermide | supplier | SIRT inhibitor | CAS [1105698-15-4] | Histone | SIRT | Inhibitor | Enzymes | | axonmedchem |
| SirReal 2 | Axon 2453
CAS [709002-46-0]
MF C22H20N4OS2MW 420.55
Purity:
98%
Soluble in DMSO
Description
SIRT2 inhibitor (IC50 value 0.14 µM) with in vivo activity, showing >1000 fold selectivity over other Class-I sirtuins SIRT1 and SIRT3. Application of SirReal2 leads to tubulin hyperacetylation in HeLa cells and induces destabilization of the checkpoint protein BubR1.
KEYWORDS: SIRT2 inhibitor | Axon 2453 | SirReal2 | 709002-46-0 | Histone | SIRT | Inhibitor | Sirtuin | tubulin | checkpoint protein | BubR1 | | axonmedchem |
| AK 7 | Axon 2270
CAS [420831-40-9]
MF C19H21BrN2O3SMW 437.35
Purity:
100%
Soluble in DMSO
Description
Potent, brain-permeable and selective inhibitor of SIRT2 (IC50 values >50 μM, 15.5 μM, and >50 μM for SIRT1, SIRT2, and SIRT3 respectively. Treatment with AK 7 showed a SIRT2-dependent nucleo-cytoplasmic trafficking in primary striatal neurons of the master regulator of cholesterol biosynthesis, SREBP-2, and resulted in protection of neurons in an in vitro model of Huntington's disease (HD). AK 7 is slightly less potent in vitro than its analogue AK 1 (Axon 2269).
References
Certificates
Categories
Extra info
T.F. Outeiro et al. Sirtuin 2 inhibitors rescue alpha-synuclein-mediated toxicity in models of Parkinson's disease. Science. 2007, 317, 516-519.
R. Luthi-Carter et al. SIRT2 inhibition achieves neuroprotection by decreasing sterol biosynthesis. Proc. Natl. Acad. Sci. USA. 2010, 107, 7927-7932.
D.M. Taylor et al. A brain-permeable small molecule reduces neuronal cholesterol by inhibiting activity of sirtuin 2 deacetylase. ACS Chem. Biol. 2011, 6, 540-546.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Cycle Regulation
Cell Signaling & Oncology
CNS
Diabetes & Metabolism
Epigenetics
p53-Tumor Suppression
DNA-damage Response
EC 3.5.1.98
SIRT
Potent, brain-permeable and selective inhibitor of SIRT2
Chemical name
3-(azepan-1-ylsulfonyl)-N-(3-bromophenyl)benzamide
Parent CAS No.
[420831-40-9]
Order
Size
Unit Price
Stock
10 mg
€90.00
In Stock | | axonmedchem |
| AK 1 | Axon 2269
CAS [330461-64-8]
MF C19H21N3O5SMW 403.45
Purity:
100%
Soluble in DMSO
Description
Potent inhibitor of SIRT with good selectivity for SIRT2 over SIRT1 and SIRT3 (IC50 values >50 μM, 12.5 μM, and >50 μM for SIRT1, SIRT2, and SIRT3 respectively. Short-term treatment with AK 1 produced large statistically significant changes in RNA expression in untransduced, Htt171-18Q- and Htt171-82Q-expressing neurons and confirm the hypothesis that AK 1-mediated neuroprotection is correlated with the negative regulation of sterol biosynthesis.AK 1 is among the first brain-permeable SIRT2 inhibitors that mediate neuroprotective reduction of cholesterol biosynthesis in an in vitro Huntington’s disease model. More potent in vitro than its analogue AK 7 (Axon 2270).
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Extra info
T.F. Outeiro et al. Sirtuin 2 inhibitors rescue alpha-synuclein-mediated toxicity in models of Parkinson's disease. Science. 2007, 317, 516-519.
R. Luthi-Carter et al. SIRT2 inhibition achieves neuroprotection by decreasing sterol biosynthesis. Proc. Natl. Acad. Sci. USA. 2010, 107, 7927-7932.
D.M. Taylor et al. A brain-permeable small molecule reduces neuronal cholesterol by inhibiting activity of sirtuin 2 deacetylase. ACS Chem. Biol. 2011, 6, 540-546.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Cycle Regulation
Cell Signaling & Oncology
CNS
Diabetes & Metabolism
Epigenetics
p53-Tumor Suppression
DNA-damage Response
EC 3.5.1.98
SIRT
Potent inhibitor of SIRT with good selectivity for SIRT2 over SIRT1 and SIRT3
Chemical name
3-(azepan-1-ylsulfonyl)-N-(3-nitrophenyl)benzamide
Parent CAS No.
[330461-64-8]
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10 mg
€90.00
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