CB1-IN-1(BPRCB1184)|CAS 1429239-98-4

Cas No.:	1429239-98-4
Synonyms:	DBPR 211,DBPR-211;DBPR211
SMILES:	C1CCN(CC1)NC(=O)C2=NN(C(=C2CNS(=O)(=O)N3CCCC3)C4=CC=C(S4)C#CC5=CC=C(C=C5)C(F)(F)F)C6=C(C=C(C=C6)Cl)Cl
Formula:	C₃₃H₃₁Cl₂F₃N₆O₃S₂
M.Wt:	750.12
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Publication:	[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 antagonist with significant weight-loss efficacy in diet-induced obese mice. J Med Chem. 2013 Dec 27;56(24):9920-9933.

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.
Target:	IC50 value: 0.3 nM (Ki, CB1R) 21 nM (Ki, CB2R) Target: CB1R
In 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.
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

Cat. No.	Product name	Field of application
DC28290	TM38837	TM38837 is a peripheral selective cannabinoid receptor type 1 (CB1) receptor antagonist. TM38837 shows limited penetrance to the brain in order to minimize or prevent CNS adverse reactions, and preserves potential antiobesity effects. TM38837 reduces propensity for psychiatric side effects.
DC8876	Rimonabant(SR141716)	Rimonabant(SR141716) is a selective central cannabinoid (CB1) receptor inverse agonist with Ki of 1.8 nM.
DC9383	Rimonabant (Hydrochloride)	Rimonabant Hcl(SR141716A) is a selective central cannabinoid (CB1) receptor inverse agonist with Ki of 1.8 nM.
DC11330	LY320135	LY320135 is a selective cannabinoid (CB) receptor 1 antagonist (Kis = 224 and >10,000 nM for CB1 and CB2, respectively, in vitro).
DC7790	CB1-IN-1(BPRCB1184)	CB1-IN-1 (BPRCB1184) 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: CB1R in 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.
DC8765	AM251	AM251 is a potent CB1 receptor antagonist (IC50 = 8 nM, Ki = 7.49 nM) that displays 306-fold selectivity over CB2 receptors; also potent GPR55 agonist (EC50 = 39 nM).