CB1-IN-1是一种新型外周大麻素-1受体(CB1R)拮抗剂，作用于CB1R(EC50=3nM)和CB2R,Ki值分别为0.3nM和21nM。
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.
[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
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