YM17E
- Product Name
- YM17E
- CAS No.
- 124900-72-7
- Chemical Name
- YM17E
- Synonyms
- YM17E;YM17E, 10 mM in DMSO;1,1'-(1,3-Phenylenebis(methylene))bis(1-cycloheptyl-3-(4-(dimethylamino)phenyl)urea);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
- CBNumber
- CB01346334
- Molecular Formula
- C40H56N6O2
- Formula Weight
- 652.93
- MOL File
- 124900-72-7.mol
YM17E Property
- 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
N-Bromosuccinimide Price
- Product number
- CS-6836
- Product name
- YM17E
- Purity
- 97.11%
- Packaging
- 1mg
- Price
- $543
- Updated
- 2021/12/16
YM17E Chemical Properties,Usage,Production
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
YM17E Preparation Products And Raw materials
Raw materials
Preparation Products
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