CP 640186 CP 640186;(R)-anthracen-9-yl(3-(morpholine-4-carbonyl)-[1,4'-bipiperidin]-1'-yl)metha none CP640186;CP 640186 (R)-ANTHRACEN-9-YL(3-(MORPHOLINE-4-CARBONYL)-1,4'-BIPIPERIDIN-1'-YL)METHANONE.HCL 591778-68-6
CP-640186 is an isozyme-nonselective acetyl-CoA carboxylase (ACCase) 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 ~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 ~30 mg/kg [1].
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