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  • GSK2190915 sodium salt
    • Fiboflapon sodium;Fiboflapon sodium
    货号: abs818768
    CAS号: 1196070-26-4
    分子式: C38H42N3NaO4S
    分子量: 659.81
    产品说明书
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    货号-规格 货期 价格 数量
    abs818768-2mg 1-2周 ¥1482.00
    - +
    abs818768-5mg 1-2周 ¥2223.00
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    大包装询价
    产品描述
    描述

    Fiboflapon sodium (GSK2190915 (sodium salt)) 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
    Fiboflapon sodium;Fiboflapon sodium
    可溶性/溶解性
    DMSO : ≥ 32 mg/mL (48.50 mM)
    生物活性
    靶点
    FLAP
    In vitro(体外研究)
    Fiboflapon (AM803) exhibits excellent preclinical toxicology and pharmacokinetics in rat and dog. Fiboflapon (AM803) also demonstrated an extended pharmacodynamic effect in a rodent bronchoalveolar lavage (BAL) model. Oral administration of Fiboflapon (AM803) (1 mg/kg) resulted 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 were challenged in vivo with calcium-ionophore, Fiboflapon (AM803) inhibited 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 (AM803) dose-dependently reduced LTB4, CysLTs, plasma protein extravasation and neutrophil influx induced by peritoneal zymosan injection. Finally, AM803 increased survival time in mice exposed to a lethal intravenous injection of platelet activating factor (PAF).
    参考文献
    参考文献
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