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.1,2 CAY10486 inhibits human ACAT-1 and ACAT-2 equally with an IC50 of approximately 60 µM.3 It also inhibits copper-mediated oxidation of low density lipoproteins by about 28% at a concentration of 3 µM.3
1
Rudel, L.L., Lee, R.G., and Cockman, T.L. Acyl coenzyme A: Cholesterol acyltransferase types 1 and 2: structure and function in atherosclerosis. Curr Opin Lipidol12121-127(2001).
2
Lee, R.G., Willingham, M.C., Davis, M.A., et al. Differential expression of ACAT1 and ACAT2 among cells within liver, intestine, kidney, and adrenal of nonhuman primates. J Lipid Res411991-2001(2000).
3
Lee, S., Han, J., Kim, H., et al. Synthesis of cinnamic acid derivatives and their inhibitory effects on LDL-oxidation, acyl-CoA: Cholesterol acyltransferase-1 and -2 activity, and decrease of HDL-particle size. Bioorg Med Chem Lett144677-4681(2004).
Rudel, L.L., Lee, R.G., and Cockman, T.L. Acyl coenzyme A: Cholesterol acyltransferase types 1 and 2: structure and function in atherosclerosis. Curr Opin Lipidol12121-127(2001).
Lee, R.G., Willingham, M.C., Davis, M.A., et al. Differential expression of ACAT1 and ACAT2 among cells within liver, intestine, kidney, and adrenal of nonhuman primates. J Lipid Res411991-2001(2000).
Lee, S., Han, J., Kim, H., et al. Synthesis of cinnamic acid derivatives and their inhibitory effects on LDL-oxidation, acyl-CoA: Cholesterol acyltransferase-1 and -2 activity, and decrease of HDL-particle size. Bioorg Med Chem Lett144677-4681(2004).
CAY10486 is available in the following screening
library: