615264-52-3

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. CAY10486 inhibits human ACAT-1 and ACAT-2 equally with an IC₅₀ value of approximately 60 μM. It also inhibits copper-mediated oxidation of low density lipoproteins by about 28% at a concentration of 3 μM.

LDL-IN-1 (Compound 1) is an antioxidant, and is active against copper mediated LDL oxidation (IC50 = 52 μM). LDL-IN-1 is also an Acyl-CoA:cholesterol acyltransferase-1 and -2 (ACAT-1/2) inhibitor, with IC50s of 60 μM. LDL-IN-1 can be used for anti-atherosclerotic research[1].

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[1] Lee S, 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 Lett. 2004 Sep 20;14(18):4677-81. DOI:10.1016/j.bmcl.2004.06.101