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JD-5037 is a cannabinoid-1 receptor blocker (CB1R antagonist) with IC50 of 1.5 nM. JD-5037 is very selective for the CB1 subtype, with a Ki of 0.35nM, >700-fold higher affinity than it has for CB2 receptors. In vivo, JD5037 (3 mg/kg/d, i.p.) induces equal reductions in body weight, attenuates the HFD-induced hyperglycemia, and 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.
| Molecular Weight | 572.51 |
| Formula | C27H27Cl2N5O3S |
| CAS Number | 1392116-14-1 |
| Solubility (25°C) | DMSO ≥ 90 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[3] Robert J Chorvat, et al. Bioorg Med Chem Lett. Peripherally restricted CB1 receptor blockers
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