Acyl-coenzyme A: cholesterol acyltransferase-1 and -2 (ACAT-1 and ACAT-2) 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. CAY10485 inhibits human ACAT-1 and ACAT-2 with an IC50 values of 95 and 81 μM, respectively. It also inhibits copper-mediated oxidation of low density lipoproteins by 91% at a concentration of 2 μM.