YM17E

Research use only, not for human use.

YM17E is an inhibitor of ACAT with IC50 of 44 nM in rabbit liver microsomes in vitro.

YM17E is an inhibitor of ACAT with IC50 of 44 nM in rabbit liver microsomes in vitro.(In Vitro):YM17E is potent in inhibiting ACAT activity in the intestine with IC50 of 34 nM.(In Vivo):YM17E inhibits the production of [14C]cholesteryloleate from [14C]oleoyl CoA in a dose-dependent manner in both liver and intestinal microsomes used as enzyme sources. YM17E (3, 5, 10 mg/kg, i.v.) significantly inhibits hepatic ACAT activities in a dose-dependent manner. YM17E (oral; i.v.) produces a significant increase in 125I-LDL clearance in atherogenic diet-fed rats. YM17E (3, 10, 30 mg/kg; p.o.) decreases total cholesterol, cholesteryl ester, and non-HDL cholesterol in a dose-dependent manner. YM17E (oral) decreases total cholesterol and cholesteryl ester levels in the liver significantly in a dose-dependent manner.

YM17E is as potent in inhibiting ACAT activity in the liver as in the intestine, with IC50 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 125I-LDL clearance in atherogenic diet-fed rats after both oral and intravenous administration. 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.

——

Others

Other Targets

HCV

——

——

124900-72-7

652.928

C40H56N6O2

>98% (HPLC)

In Vitro:?DMSO : ≥ 125 mg/mL (191.45 mM)

CN(C)c1ccc(NC(=O)N(Cc2cccc(CN(C3CCCCCC3)C(=O)Nc3ccc(cc3)N(C)C)c2)C2CCCCCC2)cc1

——

(-20℃)

With Ice Pack

≥ 2 years