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A922500
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
A922500图片
CAS NO:959122-11-3
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)428.48
FormulaC26H24N2O4
CAS No.959122-11-3
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 86 mg/mL (200.7 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)15% Captisol: 20mg/mL
SynonymsA-922500; A922500; A 922500;
实验参考方法
In Vitro

In vitro activity: A 922500 inhibits the phylogenetic family members acyl coenzyme A cholesterol acyltransferase-1 and -2 with IC50 of 296 μM. A 922500 potently inhibits huDGAT-1 and mseDGAT-1.

In VivoZucker fatty rats and diet-induced dyslipidemic hamsters are dosed orally with A 922500 (0.03, 0.3, and 3 mg/kg) for 14 days. Serum triglycerides ae significantly reduced by the 3 mg/kg dose of A 922500 in both the Zucker fatty rat (39%) and hyperlipidemic hamster (53%). These serum triglyceride changes are accompanied by significant reductions in free fatty acid levels by 32% in the Zucker fatty rat and 55% in the hyperlipidemic hamster. In addition, high-density lipoprotein-cholesterol is significantly increases (25%) in the Zucker fatty rat by A 922500 administered at 3 mg/kg. A 922500 confers weight loss and a reduction in liver triglycerides when dosed chronically in DIO mice and depletes serum triglycerides following a lipid challenge in a dose-dependent manner, thus, reproducing major phenotypical characteristics of DGAT-1(-/-) mice. A 922500 (0.03, 0.3 and 3 mg/kg, p.o.) dose-dependently attenuates the maximal postprandial rise in serum triglyceride concentrations.
Animal modelMale Golden Syrian hamsters with hyperlipidemia, and Male Zucker fatty rats
Formulation & DosageDissolved in Polyethylene glycol/hydroxypropyl-β-cyclodextrin (10% w/v); 0.03, 0.3, and 3 mg/kg; oral gavage
References

J Pharmacol Exp Ther. 2009 Aug;330(2):526-31; J Med Chem. 2008 Feb 14;51(3):380-3; Eur J Pharmacol. 2010 Jul 10;637(1-3):155-61.