Shanghai Nianxing Industrial Co., Ltd
China
Product Name: YM17E
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Purity: 97.0%
Stocking Period: 10 Day
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124900-72-7

124900-72-7 structure

124900-72-7 structure

Name: YM17E
Chemical Name: YM17E
CAS Number: 124900-72-7
Molecular Formula: C₄₀H₅₆N₆O₂
Molecular Weight: 652.912
Catalog: Signaling Pathways Metabolic Enzyme/Protease Acyltransferase
Create Date: 2018-03-20 20:51:51
Modify Date: 2024-03-11 08:21:20
YM17E is an inhibitor of acyl CoA:cholesterol acyltransferase (ACAT), with IC50 of 44 nM in rabbit liver microsomes in vitro.

Name	YM17E
Synonyms	Urea, N,N''-[1,3-phenylenebis(methylene)]bis[N-cycloheptyl-N'-[4-(dimethylamino)phenyl]- 1,1'-[1,3-Phenylenebis(methylene)]bis{1-cycloheptyl-3-[4-(dimethylamino)phenyl]urea}

Description	YM17E is an inhibitor of acyl CoA:cholesterol acyltransferase (ACAT), with IC50 of 44 nM in rabbit liver microsomes in vitro.
Related Catalog	Signaling Pathways >> Metabolic Enzyme/Protease >> Acyltransferase Research Areas >> Metabolic Disease
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].
Animal Admin	YM17E is administered to rats fed an atherogenic diet at intravenous doses of 0, 3, 5 and 10 mg/kg per day for 5 days or oral doses of 0, 3, 10 and 30 mg/kg per day for 5 days. At 2 h after final administration, all the blood and liver are removed. Serum is obtained from the blood by centrifugation and serum total cholesterol and free cholesterol are measured by an enzymatic method. Serum HDL is prepared by the heparin-Mn method.
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. [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.

Density	1.2±0.1 g/cm3
Boiling Point	862.7±65.0 °C at 760 mmHg
Molecular Formula	C₄₀H₅₆N₆O₂
Molecular Weight	652.912
Flash Point	475.5±34.3 °C
Exact Mass	652.446472
LogP	8.77
Vapour Pressure	0.0±3.3 mmHg at 25°C
Index of Refraction	1.620
Storage condition	2-8℃