K-604 is a potent, selective and competitive ACAT-1 inhibitor with IC50 of 0.45 uM for human ACAT-1, displays 229-fold selectivity over ACAT-2.
K-604 inhibits cholesterol esterification in human monocyte-derived macrophages with IC50 of 60 nM, enhances cholesterol efflux from THP-1 macrophages to HDL3 or apolipoprotein A-I.
K-604 suppresses the development of atherosclerosis in an animal model without affecting plasma cholesterol levels.
