124900-72-7
124900-72-7 结构式
基本信息
化合物 T13373
Urea, N,N''-[1,3-phenylenebis(methylene)]bis[N-cycloheptyl-N'-[4-(dimethylamino)phenyl]- (9CI)
物理化学性质
常见问题列表
IC50: 44 nM (ACAT in rabbit liver microsomes)
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.
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.