YM17E

YM17E is an inhibitor of acyl CoA:cholesterol acyltransferase ( ACAT ), with IC 50 of 44 nM in rabbit liver microsomes in vitro. In Vitro YM17E is as potent in inhibiting ACAT activity in the liver as in the intestine, with IC 50 values of 45 and 34 nM, respectively. MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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 125 I-LDL clearance in atherogenic diet-fed rats after both oral and intravenous administration . YM17E inhibits production of [ 14 C]cholesteryloleate from [ 14 C]oleoyl CoA in a dose-dependent manner in both liver and intestinal microsomes used as enzyme sources. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:IC50: 44 nM (ACAT in rabbit liver microsomes)

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