K-604, ACAT-1 Inhibitor

K-604 is an inhibitor of acyl-CoA:cholesterol acyltransferase 1 (ACAT1). The IC₅₀ values of K-604 for human ACAT-1 and ACAT-2 are 0.45 μM and 102.85 μM respectively, showing that K-604 is 229-fold more selective for ACAT-1. It suppresses the development of atherosclerosis in an animal model without affecting plasma cholesterol levels. It stimulates collagen production in cultured smooth muscle cells and modulates plaque phenotype in apolipoprotein E-knockout mice.