JD5037 是一种 CB1R 有效拮抗剂，IC50=1.5 nM。

JD-5037 is a novel, peripherally restricted CB1R antagonist with an IC50 of 1.5 nM.

JD5037 (3 mg/kg/d, i.p.) induces equal reductions in body weight, attenuates the HFD-induced hyperglycemia as well as reduces the HFD-induced hepatic injury and steatosis in obese Magel2-null mice. JD5037 (3 mg/kg/day, p.o.) significantly reduces the size of tumors and abrogates the tumor in DEN-treated mice. JD5037 attenuates the AEA levels in HCC samples from mice.

Mice: JD-5037 is formulated in vehicle (V; 1% Tween80, 4% DMSO, 95% Saline). Obese mice are treated chronically (28 d) with vehicle (V; 1% Tween80, 4% DMSO, 95% Saline), JD5037, or SLV319 at a dose of 3 mg/kg, i.p. Body weight and food intake are monitored daily. Mice are euthanized by cervical dislocation under anesthesia; the brain, hypothalamus, liver, and combined fat pads are removed, weighed, and snap-frozen, and trunk blood is collected for determining the endocrine and biochemical parameters

1392116-14-1

C27H27Cl2N5O3S

572.51

JD 5037

DMSO:10 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years