[CAS NO. 124900-72-7] YM17E
PRODUCTS SPECIFICATIONS [124900-72-7]
DESCRIPTION [124900-72-7]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 652.91 |
| Molecular Formula | C40H56N6O2 |
| SMILES | O=C(NC1=CC=C(N(C)C)C=C1)N(CC2=CC=CC(CN(C3CCCCCC3)C(NC4=CC=C(N(C)C)C=C4)=O)=C2)C5CCCCCC5 |
Summary
YM17E is an inhibitor of acyl CoA:cholesterol acyltransferase ( ACAT ), with IC 50 of 44 nM in rabbit liver microsomes in vitro.
IC50 & 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 IC 50 values of 45 and 34 nM, respectively [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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 125 I-LDL clearance in atherogenic diet-fed rats after both oral and intravenous administration [1] . YM17E inhibits production of [ 14 C]cholesteryloleate from [ 14 C]oleoyl CoA in a dose-dependent manner in both liver and intestinal microsomes used as enzyme sources [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : ≥ 125 mg/mL ( 191.45 mM )
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.5316 mL | 7.6580 mL | 15.3160 mL |
| 5 mM | 0.3063 mL | 1.5316 mL | 3.0632 mL |
| 10 mM | 0.1532 mL | 0.7658 mL | 1.5316 mL |
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.
