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  • A-922500
    • A 922500;DGAT-1 Inhibitor 4a
    货号: abs813326
    CAS号: 959122-11-3
    分子式: C26H24N2O4
    分子量: 428.48
    产品说明书
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    货号-规格 货期 价格 数量
    abs813326-5mg 1-2周 ¥1325.00
    - +
    abs813326-10mg 1-2周 ¥1877.00
    - +
    abs813326-50mg 1-2周 ¥5989.00
    - +
    大包装询价
    产品描述
    描述

    A-922500是人类和小鼠DGAT-1抑制剂,IC50分别为7 nM和24 nM,比作用于相关的酰基转移酶,hERG及抗靶面板的选择性高。

    纯度
    >98%
    储存/保存方法
    store at -20℃ for one year(Powder);
    in DMSO or others solvent store at 2-4℃ for two weeks, at -20℃ for six months.
    基本信息
    别名
    A 922500;DGAT-1 Inhibitor 4a
    可溶性/溶解性
    DMSO :21.4 mg/mL (50 mM)
    生物活性
    靶点
    human DGAT-1 ,mouse DGAT-1
    In vitro(体外研究)
    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 vivo(体内研究)
    Zucker 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.
    参考文献
    参考文献
    Diacylglycerol acyltransferase 1 inhibition lowers serum triglycerides in the Zucker fatty rat and the hyperlipidemic hamster.
    King AJ, et al. J Pharmacol Exp Ther. 2009 Aug;330(2):526-31. PMID: 19478132.
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