E-5324 is potent cholesterol acyltransferase (ACAT) inhibitor (IC50s: 44 to 190 nM).

ACAT:44 to 190 nM

E-5324 inhibits the incorporation of [3H]oleate into cholesteryl [3H]oleate in a concentration-dependent manner (IC50: 0.44 μM) and it also inhibits [3H]cholesteryl ester synthesis (IC50: 0.41 μM). E-5324 displays no effect on triglyceride synthesis up to 10 μM and it also has no effect on bovine pancreatic cholesterol esterase or lecithin: cholesterol acyltransferase (LCAT) up to 10 μM [1].

E-5324 treatment significantly decreases the wet weight and protein content. The high dose of E-5324 (0.1%) obviously decreases the surface involvement by 34% and 54% in the aortic arch and thoracic aorta, respectively. In the aortic arch, the high dose of E-5324 (0.1%) obviously reduces both cholesteryl ester and total cholesterol by 60% and 59%, respectively. The high dose of E-5324 (0.1%) markedly decreases the ACAT activities in the aortic arch and thoracic aorta by 35% and 44%, respectively. The areas under the cholesterol-time curves for duration of this study (AUC) for control, E-5324 0.02% and E-5324 0.1% are 104985±4411, 106096±4476 and 105231±4 348 mg×day/dL, respectively [2].