CB1-IN-1

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.

Product Specifications

CAS Number

[1429239-98-4]

Product Name Alternative

BPRCB1184

UNSPSC

12352005

Hazard Statement

H302, H315, H319

Target

Cannabinoid Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein; Neuronal Signaling

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/CB1-IN-1.html

Concentration

10mM

Purity

99.83

Solubility

DMSO : 125 mg/mL (ultrasonic)

Smiles

ClC1=CC(Cl)=CC=C1N2C(C3=CC=C(C#CC4=CC=C(C(F)(F)F)C=C4)S3)=C(CNS(=O)(N5CCCC5)=O)C(C(NN6CCCCC6)=O)=N2

Molecular Formula

C33H31Cl2F3N6O3S2

Molecular Weight

751.67

Precautions

H302, H315, H319

References & Citations

[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.