Identification | Back Directory | [Name]
YM17E | [CAS]
124900-72-7 | [Synonyms]
YM17E Urea, N,N''-[1,3-phenylenebis(methylene)]bis[N-cycloheptyl-N'-[4-(dimethylamino)phenyl]- (9CI) | [Molecular Formula]
C40H56N6O2 | [MOL File]
124900-72-7.mol | [Molecular Weight]
652.91 |
Chemical Properties | Back Directory | [Boiling point ]
862.7±65.0 °C(Predicted) | [density ]
1.16±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
Soluble in DMSO | [form ]
Solid | [pka]
14.03±0.70(Predicted) | [color ]
White to off-white |
Hazard Information | Back Directory | [Uses]
YM17E is an inhibitor of acyl CoA:cholesterol acyltransferase (ACAT), with IC50 of 44 nM in rabbit liver microsomes in vitro. | [Biological Activity]
YM17E is an inhibitor of acyl-CoA:cholesterol acyltransferase (ACAT) with IC50 of 44 nM in vitro in rabbit liver microsomes. | [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. | [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]. | [target]
IC50: 44 nM (ACAT in rabbit liver microsomes) | [storage]
Store at -20°C | [References]
[1] Uchida T, et al. Relationship between bioavailability and hypocholesterolemic activity of YM17E, an inhibitor of ACAT, in cholesterol-fed rats. Atherosclerosis. 1998 Mar;137(1):97-106. DOI:10.1016/s0021-9150(97)00259-1 [2] Kashiwa M, et al. Pharmacological properties of YM17E, an acyl-CoA:cholesterol acyltransferase inhibitor, and diarrheal effect in beagle dogs. Jpn J Pharmacol. 1997 Jan;73(1):41-50. DOI:10.1254/jjp.73.41 |
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cjbscvictory
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13348960310 13348960310 |
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https://www.weikeqi-biotech.com/ |
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