YM17E

YM17E is an inhibitor of acyl CoA:cholesterol acyltransferase (ACAT), with IC₅₀ of 44 nM in rabbit liver microsomes in vitro. IC50 & Target: IC50: 44 nM (ACAT in rabbit liver microsomes)^[1] In Vitro: YM17E is as potent in inhibiting ACAT activity in the liver as in the intestine, with IC₅₀ values of 45 and 34 nM, respectively^[2]. In Vivo: YM17E (3, 10 and 30 mg/kg per day, p.o.) decreases total cholesterol, cholesteryl ester and non-HDL cholesterol in a dose-dependent manner. Total cholesterol and cholesteryl ester levels in liver do not decrease significantly after intravenous administration of YM17E, but do decrease significantly and in a dose-dependent manner after oral administration. YM17E (3, 5, 10 mg/kg, i.v.) significantly inhibits hepatic ACAT activities in a dose-dependent manner. YM17E produces a significant increase in ¹²⁵I-LDL clearance in atherogenic diet-fed rats after both oral and intravenous administration^[1]. YM17E inhibits production of [¹⁴C]cholesteryloleate from [¹⁴C]oleoyl CoA in a dose-dependent manner in both liver and intestinal microsomes used as enzyme sources^[2].