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  • GSK2190915

    • AM-803; Fiboflapon; GSK-2190915
    货号: abs819530
    CAS号: 936350-00-4
    分子式: C38H43N3O4S
    分子量: 637.83
    产品说明书
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    货号-规格 货期 价格 数量
    abs819530-2mg 1-2周 ¥2037.00
    - +
    abs819530-5mg 1-2周 ¥3057.00
    - +
    abs819530-10mg 1-2周 ¥5094.00
    - +
    大包装询价
    产品描述
    描述

    GSK2190915(AM-803; Fiboflapon) is a potent FLAP(5-Lipoxygenase-activating protein) inhibitor with binding IC50 of 2.9 nM.

    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
    AM-803; Fiboflapon; GSK-2190915
    可溶性/溶解性
    DMSO : 50 mg/mL (78.39 mM; Need ultrasonic)
    生物活性
    靶点
    FLAP
    In vitro(体外研究)
    Fiboflapon (AM-803) exhibits excellent preclinical toxicology and pharmacokinetics in rat and dog. Fiboflapon (AM-803) also demonstrated an extended pharmacodynamic effect in a rodent bronchoalveolar lavage (BAL) model.
    In vivo(体内研究)
    Oral administration of Fiboflapon (AM-803: 1 mg/kg) results in sustained inhibition of ex vivo ionophore-challenged whole blood LTB4 biosynthesis with >90% inhibition for up to 12 h and an EC50 of approximately 7 nM. When rat lungs are challenged in vivo with calcium-ionophore, Fiboflapon (AM-803) inhibits LTB4 and cysteinyl leukotriene (CysLT) production with ED50s of 0.12 mg/kg and 0.37 mg/kg, respectively. The inhibition measured 16 h following a single oral dose of 3 mg/kg was 86% and 41% for LTB4 and CysLTs, respectively. In an acute inflammation setting, Fiboflapon dose-dependently reduced LTB4, CysLTs, plasma protein extravasation and neutrophil influx induced by peritoneal zymosan injection. Finally, Fiboflapon increases survival time in mice exposed to a lethal intravenous injection of platelet activating factor (PAF).
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    • 实验方法 实验条件
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