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  • Darapladib

    • SB-480848;达拉地
    货号: abs813081
    CAS号: 356057-34-6
    分子式: C36H38F4N4O2S
    分子量: 666.780
    产品说明书
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    货号-规格 货期 价格 数量
    abs813081-5mg 1-2周 ¥1142.00
    - +
    abs813081-10mg 1-2周 ¥1902.00
    - +
    abs813081-25mg 1-2周 ¥3993.00
    - +
    大包装询价
    产品描述
    描述

    Darapladib (SB-480848) is a reversible lipoprotein-associated phospholipase A2 (Lp-PLA2) inhibitor with IC50 of 0.25 nM. Phase 3.

    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
    SB-480848;达拉地
    可溶性/溶解性
    Ethanol :93 mg/mL (139.5 mM)

    DMSO :93 mg/mL (139.5 mM)
    生物活性
    靶点
    Phospholipase
    In vitro(体外研究)
    Mechanistic studies using steady state and transient kinetics indicate Darapladib (SB-480848) to be a freely reversible, non-covalently bound, inhibitor of rhLp-PLA2 with a Ki of 110 pM and an off-rate of 27 min. Potent inhibition of the enzyme in whole human plasma is confirmed (IC50=5±2 nM). Furthermore, the presence of Darapladib during the copper catalysed oxidation of human LDL prevents the production of lyso-PtdCho (IC50=4±3 nM) and subsequent monocyte chemotaxis (IC50=4±1 nM).
    In vivo(体内研究)
    Additional in vivo studies with Darapladib indicated an oral bioavailability of 11±2% in the fed rat. The oral bioavailability of Darapladib is 28±4% in the dog. Furthermore excellent inhibition of Lp-PLA2 within the atherosclerotic plaque is achieved for Darapladib, with 95±1% inhibition observed 2 h after an oral dose of 30 mg/kg to the WHHL rabbit. Darapladib, a specific inhibitor of lipoprotein-associated phospholipase A2 (lp-PLA2), on inflammation and atherosclerotic formation in the low density lipoprotein receptor (LDLR)-deficient mice. the activity of serum lp-PLA2 is inhibited by more than 60% in LDLR-deficient mice after oral administration of 50 mg/kg once daily of Darapladib for 6 weeks. Darapladib significantly inhibits serum lp-PLA2 activity in LDLR-deficient mice.
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    • 实验方法 实验条件
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