JD5037

Description: JD5037 is a novel and potent inverse agonist of peripherally restricted (PR) cannabinoid 1 (CB1) receptors with Ki of 0.35 nM. Antagonists (inverse agonists) of the cannabinoid-1 (CB1) receptor showed promise as new therapies for controlling obesity and related metabolic function/liver disease. These agents, representing diverse chemical series, shared the property of brain penetration due to the initial belief that therapeutic benefit was mainly based on brain receptor interaction. JD5037 displays > 700-fold selectivity for CB1 over CB2, > 1, 000-fold selectivity over a panel of 70 receptors, transporters, and ion channels, and low blood-brain barrier penetrance.JD5037 is orally bioavailable and reduces food intake, body weight, and hormonal/metabolic abnormalities in diet-induced obese mice.

References: Mol Metab. 2016 Oct 22; 5(12):1187-1199. eCollection 2016 Dec.

JD-5037; JD 5037; JD5037;

Chemical Name: (S)-2-(((E)-((S)-3-(4-chlorophenyl)-4-phenyl-4, 5-dihydro-1H-pyrazol-1-yl)((4-chlorophenyl)sulfonamido)methylene)amino)-3-methylbutanamide

Exact Mass: 571.1212