Basic information Safety Supplier Related

YM17E

Basic information Safety Supplier Related

YM17E Basic information

Product Name:
YM17E
Synonyms:
  • YM17E
  • Urea, N,N''-[1,3-phenylenebis(methylene)]bis[N-cycloheptyl-N'-[4-(dimethylamino)phenyl]- (9CI)
  • Diglyceride acyltransferase,Inhibitor,acyl-CoA:cholesterol acyltransferase,inhibit,YM17E,Acyltransferase,Diacylglycerol acyltransferase,mono- acylglycerol acyltransferase,YM-17E
  • 1,1'-(1,3-Phenylenebis(methylene))bis(1-cycloheptyl-3-(4-(dimethylamino)phenyl)urea)
  • YM17E, 10 mM in DMSO
CAS:
124900-72-7
MF:
C40H56N6O2
MW:
652.93
Mol File:
124900-72-7.mol
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YM17E Chemical Properties

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
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YM17E Usage And Synthesis

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)

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

YM17ESupplier

Shanghai YuanYe Biotechnology Co., Ltd.
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021-61312847; 18021002903
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Tianjin Kailiqi Biotechnology Co., Ltd.
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15076683720
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klq@cw-bio.com
Fan De(Beijing) Biotechnology Co., Ltd.
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15911056312
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liming@bio-fount.com
TargetMol Chemicals Inc.
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+1-781-999-5354; +17819995354
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ChemeGen(Shanghai) Biotechnology Co.,Ltd.
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18818260767
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