CP-640186 (hydrochloride)

591778-70-0

C30H36ClN3O3

DMSO : >= 48 mg/mL (91.94 mM)

Metabolic Enzyme/Protease

CP-640186 Hcl is an isozyme-nonselective acetyl-CoA carboxylase (ACC) inhibitor with IC50s of 53 nM and 61 nM for rat liver ACC1 and rat skeletal muscle ACC2 respectively; with improved metabolic stability vs CP-610431. IC50 value: 53 nM/61 nM (rat liver ACC1/skeletal muscle ACC2) [1] Target: acetyl-CoA carboxylase in vitro: CP-640186, also inhibited both isozymes with IC50s of ca.55 nM but was 2�3 times more potent than CP-610431 in inhibiting HepG2 cell fatty acid and TG synthesis. CP-640186 also stimulated fatty acid oxidation in C2C12 cells (ACC2) and in rat epitrochlearis muscle strips with EC50s of 57 nM and 1.3 uM [1]. in vivo: In rats, CP-640186 lowered hepatic, soleus muscle, quadriceps muscle, and cardiac muscle malonyl-CoA with ED50s of 55, 6, 15, and 8 mg/kg. Consequently, CP-640186 inhibited fatty acid synthesis in rats, CD1 mice, and ob/ob mice with ED50s of 13, 11, and 4 mg/kg, and stimulated rat whole body fatty acid oxidation with an ED50 of ca.30 mg/kg [1].