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  • GLPG1837
  • GLPG-1837;GLPG 1837;ABBV-974; ABBV 974; ABBV974
  • 货号: abs814652
    CAS号: 1654725-02-6
    分子式: C16H20N4O3S
    分子量: 348.42
    产品说明书
    分享:
    货号-规格 货期 价格 数量
    abs814652-5mg 1-2周 ¥1680.00
    - +
    abs814652-25mg 1-2周 ¥5460.00
    - +
    大包装询价
    产品描述
    描述

    GLPG1837 is a novel CFTR potentiator with an EC50 value of 3 nM for F508del, showing enhanced efficacy on CFTR mutants harboring class III mutations compared to Ivacaftor.

    纯度
    >98%
    储存/保存方法
    Store at -20°C
    基本信息
    别名
    GLPG-1837;GLPG 1837;ABBV-974; ABBV 974; ABBV974
    外观
    powder
    可溶性/溶解性
    DMSO:69 mg/mL (198.04 mM)

    Ethanol :5 mg/mL (14.35 mM)
    生物活性
    靶点
    CFTR(F508del),CFTR(G551D)
    In vitro(体外研究)
    GLPG1837 has an attractive in vitro ADME profile, showing low Clint,unb in both microsomal and hepatocytes stability assays, good permeability, and no off-target inhibition of CYPs and the hERG channel.
    In vivo(体内研究)
    The pharmacokinetic profile of GLPG1837 is attractive, showing a low Cl,unb and good F% in both rat and dog. The CL (L/h/kg) of GLPG1837 after intravenous injection of 1 mg/kg dose are 1.92 and 0.32 in rats and dogs, respectively. T1/2 is 1.84 h in rats while 3 h in dogs. After 5 mg/kg p.o, the oral availability of GLPG1837 in rat is 67%. In dogs, F%>100.
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