Description
YM17E is an inhibitor of acyl CoA:cholesterol acyltransferase (ACAT), with IC50 of 44 nM in rabbit liver microsomes in vitro.
Product information
CAS Number: 124900-72-7
Molecular Weight: 652.91
Formula: C40H56N6O2
Chemical Name: 1-cycloheptyl-1-({3-[(1-cycloheptyl{[4-(dimethylamino)phenyl]carbamoyl}amino)methyl]phenyl}methyl)-3-[4-(dimethylamino)phenyl]urea
Smiles: CN(C)C1C=CC(=CC=1)NC(=O)N(CC1C=C(CN(C2CCCCCC2)C(=O)NC2C=CC(=CC=2)N(C)C)C=CC=1)C1CCCCCC1
InChiKey: LZQSLXDZJBXHRS-UHFFFAOYSA-N
InChi: InChI=1S/C40H56N6O2/c1-43(2)35-24-20-33(21-25-35)41-39(47)45(37-16-9-5-6-10-17-37)29-31-14-13-15-32(28-31)30-46(38-18-11-7-8-12-19-38)40(48)42-34-22-26-36(27-23-34)44(3)4/h13-15,20-28,37-38H,5-12,16-19,29-30H2,1-4H3,(H,41,47)(H,42,48)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
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.
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. 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.
Products are for research use only. Not for human use.
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