Acyl-Coenzyme A:cholesterol acyltransferases (ACAT1 and ACAT2) catalyze the formation of cholesterol esters from cholesterol and long chain fatty acyl-coenzyme A, and may play a role in the development of atherosclerosis.{20948} Avasimibe is an orally bioavailable inhibitor of ACAT (IC50s = 24 and 9.2 µM for ACAT1 and ACAT2, respectively).{21762} It reduces foam cell formation in human macrophages in vitro, enhancing free cholesterol efflux and inhibiting the uptake of modified LDL and dose-dependently reduces plasma total triglyceride and VLDL cholesterol levels in cholesterol-fed animal models.{29393,29394} Avasimibe inhibition of ACAT has been used to decrease amyloid β generation in models of Alzheimer’s disease.{29395}
产品描述
An orally bioavailable inhibitor of ACAT (IC50s = 24 and 9.2 µM for ACAT1 and ACAT2, respectively) that reduces plasma total triglyceride and VLDL cholesterol levels in cholesterol-fed animal models; also used to decrease amyloid β generation in models of Alzheimer’s disease
