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  • 产品名称: Eliglustat hemitartrate 依利格鲁司特酒石酸盐
  • 产品货号: CST11176
  • 货期: 现货
  • 价格与订购: 1200
  • 数量:
    库存: 5
  • 规格: 100mg
  • 产品信息
  • 如何订购
    产品描述
    Eliglustat Hemitartrate, with an IC50 of 24 nM, is a specific, potent, oral active glucocerebral glycosidase inhibitor.
    体外活性
    Eliglustat tartrate shows good potency with an IC50 of 24 nM and specificity against the target enzyme.
    体内活性
    A novel inhibitor of glucosylceramide synthase (Genz-112638) and assessed its activity in a murine model of Gaucher disease (D409V/null).?Biochemical characterization of Genz-112638 showed good potency (IC(50) approximately 24nM) and specificity against the target enzyme.?Mice that received drug prior to significant accumulation of substrate (10 weeks of age) showed reduced levels of glucosylceramide and number of Gaucher cells in the spleen, lung and liver when compared to age-matched control animals.?Treatment of older mice that already displayed significant amounts of tissue glucosylceramide (7 months old) resulted in arrest of further accumulation of the substrate and appearance of additional Gaucher cells in affected organs.?These data indicate that substrate inhibition therapy with Genz-112638 represents a viable alternate approach to enzyme therapy to treat the visceral pathology in Gaucher disease.
    分子式
    C27H42N2O10
    分子量
    554.63
    别名
    Genz-112638;依利格鲁司特酒石酸盐;Eliglustat tartrate
    参考文献
    [1]McEachern KA, et al. A specific and potent inhibitor of glucosylceramide synthase for substrate inhibition therapy ofGaucher disease. Mol Genet Metab. 2007 Jul;91(3):259-67.
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    储存和溶解度
    H2O:50 mg/mL (52.13 mM)
    DMSO:50 mg/mL (52.13 mM)
    Powder: -20°C for 3 years
    In solvent: -80°C for 2 years
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    Note
    For Research Use Only.