CP-640186,591778-70-0

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CP-640186 hydrochloride

CAS No. : 591778-70-0

MCE 国际站：CP-640186 hydrochloride

产品活性：CP-640186 hydrochloride 是一种具有口服活性的、可透过细胞的乙酰-CoA 羧化酶 (ACC) 抑制剂，其对大鼠肝脏 ACC1 和大鼠骨骼肌 ACC2 的 IC₅₀s 分别为 53 nM 和 61 nM。乙酰-CoA羧化酶 (ACC) 是脂肪酸代谢的一个关键酶，能够合成丙二酰-CoA。CP-640186 hydrochloride 还可以刺激肌肉脂肪酸的氧化。

研究领域：Metabolic Enzyme/Protease

作用靶点：Acetyl-CoA Carboxylase

In Vitro: CP-640186 (20 µM; 48 h) treatment can inhibit H460 cell growth.
CP-640186 (0.1 nM-100 µM; 2 h) treatment increases fatty acid metabolism in a concentration-dependent manner in C2C12 cells and muscle strips.
CP-640186 (0.62-1.8 µM; 2 h) treatment inhibits fatty acid synthesis and TG synthesis in HepG2 cells.

In Vivo: CP-640186 (oral gavage; 4.6-21 mg/kg; once) demonstrates acute efficacy.
CP-640186 (intravenous injection and oral gavage; Intravenous dose, 5 mg/kg; oral dose, 10 mg/kg; once) shows lowe drug exposure in the rat than the ob/ob mouse at equal doses.
CP-640186 (oral gavage; 100 mg/kg; once) treatment shows a complete shift from carbohydrate utilization to fatty acid utilization as a source of energy at high exposure level.

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