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  • E1210
    • APX001A
    货号: abs819625
    CAS号: 936339-60-5
    分子式: C21H18N4O2
    分子量: 358.39
    产品说明书
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    货号-规格 货期 价格 数量
    abs819625-5mg 1-2周 ¥1575.00
    - +
    abs819625-25mg 1-2周 ¥6825.00
    - +
    大包装询价
    产品描述
    描述
    E1210 is a first-in-class, broad-spectrum and orally active antifungal. E1210 has a mechanism of action-inhibition of fungal glycosylphosphatidylinositol (GPI) biosynthesis.
    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
    中文别名
    APX001A
    可溶性/溶解性
    DMSO : 250 mg/mL (697.56 mM; Need ultrasonic)
    生物活性
    靶点
    Fungal
    In vitro(体外研究)
    E1210 inhibits the inositol acylation activity of C. albicans Gwt1p and A. fumigatus Gwt1p with IC50s of 0.3 to 0.6 μM but has no inhibitory activity against human Pig-Wp even at concentrations as high as 100 μM. To confirm the inhibition of fungal glycosylphosphatidylinositol (GPI) biosynthesis, expression of ALS1 protein, a GPI-anchored protein, on the surfaces of C. albicans cells treated with E1210 is studied and shown to be significantly lower than that on untreated cells. E1210 inhibits germ tube formation, adherence to polystyrene surfaces, and biofilm formation of C. albicans at concentrations above its MIC.
    In vivo(体内研究)
    E1210 (2.5 mg/kg, 5 mg/kg and 10 mg/kg; oral administration; twice daily; for 3 days; specific-pathogen-free female ICR mice) treatment reduces the number of viable C. albicans cells in the oral cavity in a dose-dependent manner.
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