"目录号: HY-15259A
CP-640186盐酸盐是乙酰辅酶A羧化酶（ACCase）抑制剂，对鼠肝ACCase1和骨骼肌ACCase2的IC50s分别为53 nM和61 nM，比CP-610431有着更好的代谢稳定性。
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SBE-β-CD-MPTP hydrochloride-Cyclosporin A-Etomoxir-Auranofin-GKT137831-Ceruletide-Acetylcysteine-JC-1-BPTES-Brassinolide-FCCP-IPTG-MTT-RSL3 1S,3R--
生物活性
Description
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 carboxylasein 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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