产品描述:
ETC-1002 is a prodrug form of ETC-1002-CoA.{46141} ETC-1002 is conjugated to coenzyme A (CoA) by very long-chain acyl-CoA synthetase-1 (ACSVL1) to form ETC-1002-CoA, which inhibits ATP citrate lyase (Ki = 2 μM) and activates AMP-activated protein kinase (AMPK). ETC-1002 suppresses total lipid synthesis in wild-type and AMPKβ1 knockout primary murine hepatocytes. In vivo, ETC-1002 (30 mg/kg) prevents increases in hepatic cholesterol and reduces the size of aortic atherosclerotic lesions induced by a high-fat high-cholesterol diet in Apoe-/-/Ampkβ1-/- (DKO) mice.