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  • Dicoumarol

    • 双羟香豆素;Dicumarol
    货号: abs816049
    CAS号: 66-76-2
    分子式: C19H12O6
    分子量: 336.29
    产品说明书
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    货号-规格 货期 价格 数量
    abs816049-25mg 1-2周 ¥629.00
    - +
    abs816049-50mg 1-2周 ¥1130.00
    - +
    abs816049-100mg 1-2周 ¥1467.00
    - +
    abs816049-200mg 1-2周 ¥2210.00
    - +
    大包装询价
    产品描述
    描述

    Dicoumarol is a competitive NADH quinone oxidoreductase (NQO1) inhibitor,and used as an anticoagulant by interfering with the metabolism of vitamin K.

    纯度
    99%
    储存/保存方法
    Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
    基本信息
    别名
    双羟香豆素;Dicumarol
    外观
    白色粉末
    可溶性/溶解性
    DMSO : 62 mg/mL (184.4 mM)

    Ethanol : 62 mg/mL (184.4 mM)
    生物活性
    靶点
    PDHK
    In vitro(体外研究)
    Dicoumarol is an inhibitor of both NAD(P)H:quinone oxidoreductase 1 (NQO1) and PDK1 with IC50s of 0.37±0.15 and 19.42±0.032 μM, respectively. The PDK1 activity is inhibited by Dicoumarol in a dose-dependent manner. The enzymatic activity of PDK1 is reduced by approximately 94% when treated with 200 μM Dicoumarol. Dicoumarol decreases the p-PDHA1 level by 26% (100 μM Dicoumarol) and by 72% (200 μM Dicoumarol), with no statistical difference in the total PDHA1 level. Both 100 μM and 200 μM Dicoumarol markedly induce apoptosis of SKOV3 cells. Similarly, flow cytometric analysis of annexin V+PI+ cells reveals that 100 μM and 200 μM Dicoumarol treatments generate approximately 20.87% and 24.94% apoptotic cells, respectively, significantly higher than vehicle treatment. It is also observed that treatment of MCF-7-TAMR cells with Dicoumarol, a known NQO1 inhibitor, reverses their tamoxifen-resistance phenotype.
    In vivo(体内研究)
    Dichloroacetate (DCA) at 100 mg/kg, Dicoumarol at 30 mg/kg, and Dicoumarol at 50 mg/kg all significantly reduce tumor volume and decrease tumor weight, when compare to tumors from control or vehicle groups. Total caspase-3 and total anti-poly (ADP-ribose) polymerase (PARP) are significantly decreased in Dicoumarol-treated SKOV3 xenografts, when compare to tumors from the control or vehicle group.
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    • 实验方法 实验条件
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