CB1-IN-1

Names

[ Name ]:
CB1-IN-1

[Synonym ]:
1-(2,4-Dichlorophenyl)-N-(1-piperidinyl)-4-{[(1-pyrrolidinylsulfonyl)amino]methyl}-5-(5-{[4-(trifluoromethyl)phenyl]ethynyl}-2-thienyl)-1H-pyrazole-3-carboxamide
1H-Pyrazole-3-carboxamide, 1-(2,4-dichlorophenyl)-N-1-piperidinyl-4-[[(1-pyrrolidinylsulfonyl)amino]methyl]-5-[5-[2-[4-(trifluoromethyl)phenyl]ethynyl]-2-thienyl]-
CB1-IN-1

Biological Activity

[Description]:

CB1-IN-1 is a peripherally restricted CB1R antagonist, with Ki of 0.3 nM and 21 nM for CB1R (EC50 = 3 nM) and CB2R, respectively.IC50 value: 0.3 nM (Ki, CB1R) 21 nM (Ki, CB2R)Target: CB1Rin vivo: CB1-IN-1 is a novel peripherally restricted cannabinoid 1 receptor antagonist with significant weight-loss efficacy in diet-induced obese mice. CB1-IN-1 has great potential to ameliorate this related metabolic syndrome.

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> Cannabinoid Receptor

Research Areas >> Neurological Disease

[References]

[1]. Chang CP, et al. Discovery of 1-(2,4-dichlorophenyl)-N-(piperidin-1-yl)-4-((pyrrolidine-1-sulfonamido)methyl)-5-(5-((4-(trifluoromethyl)phenyl)ethynyl)thiophene-2-yl)-1H-pyrazole-3-carboxamide as a novel peripherally restricted cannabinoid-1 receptor anta

[Related Small Molecules]

WIN 55212-2 mesylate | AM251 | Taranabant | SR144528 | Bay 59-3074 | Org 27569 | Otenabant | GW842166X | A-836339 | BML-190 | JD-5037 | (±)-SLV319 | Pregnenolone | Anandamide | 2-arachidonoylglycerol

Chemical & Physical Properties

[ Density]:
1.5±0.1 g/cm3

[ Molecular Formula ]:
C₃₃H₃₁Cl₂F₃N₆O₃S₂

[ Molecular Weight ]:
751.669

[ Exact Mass ]:
750.122803

[ LogP ]:
6.52

[ Index of Refraction ]:
1.672

[ Storage condition ]:
2-8℃

Related Compounds

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