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  • HM-30181-A

    • Encequidar;HM30181;HM30181A
    货号: abs813092
    CAS号: 849675-66-7
    分子式: C38H36N6O7
    分子量: 688.728
    产品说明书
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    货号-规格 货期 价格 数量
    abs813092-5mg 1-2周 ¥1158.00
    - +
    abs813092-10mg 1-2周 ¥1709.00
    - +
    abs813092-50mg 1-2周 ¥5237.00
    - +
    大包装询价
    产品描述
    描述

    HM-30181-A是一种有效的选择性的P-glycoprotein抑制剂。

    纯度
    98%
    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
    Encequidar;HM30181;HM30181A
    可溶性/溶解性
    DMSO : 2.4 mg/mL (3.48 mM; Need ultrasonic)
    生物活性
    靶点
    P-glycoprotein
    In vitro(体外研究)
    HM30181 is shown to be approximately equipotent with the reference Pgp inhibitor tariquidar in inhibiting rhodamine 123 efflux from CCRF-CEM T cells (IC50, tariquidar: 8.2±2.0 nM, HM30181: 13.1±2.3 nM) . HM30181 shows a high selectivity for mP-gp and its potency is 20-50 times higher than that of tariquitar, another third generation P-gp inhibitor.
    In vivo(体内研究)
    PET scans with the Pgp substrate (R)-verapamil in FVB wild-type mice pretreated i.v. with HM30181 (10 or 21 mg/kg) failes to show significant increases in (R)-verapamil brain uptake compared with vehicle treated animals. HM30181 inhibits P-gp mainly in the intestinal endothelium, which can be beneficial because pan-inhibition of P-gp, particularly in the brain, could lead to detrimental adverse events. HM30181 increases the oral bioavailability of co-administered paclitaxel by more than 12 times in rats.
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    • 实验方法 实验条件
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