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  • Empagliflozin
    • 依帕列净;恩格列净;BI-10773;BI 10773;BI10773
    货号: abs817359
    CAS号: 864070-44-0
    分子式: C23H27ClO7
    分子量: 450.91
    产品说明书
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    货号-规格 货期 价格 数量
    abs817359-5mg 现货 ¥772.00
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    abs817359-10mg 现货 ¥1048.00
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    abs817359-50mg 现货 ¥2371.00
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    abs817359-100mg 1-2周 ¥3738.00
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    大包装询价
    产品描述
    描述

    Empagliflozin (BI-10773) is a potent and selective SGLT-2 inhibitor with IC50 of 3.1 nM, exhibits >300-fold selectivity over SGLT-1, 4, 5 and 6.

    纯度
    99%
    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
    依帕列净;恩格列净;BI-10773;BI 10773;BI10773
    外观
    White to off white solid
    可溶性/溶解性
    DMSO : 83 mg/mL (184.1 mM)
    生物活性
    靶点
    SGLT2
    In vitro(体外研究)
    Empagliflozin shows >2500-fold selectivity for hSGLT-2 over hSGLT-1 (IC50 8300 nM) and >3500-fold selectivity over hSGLT-4, it exhibits >350-fold selectivity over hSGLT-5 (IC50=1100 nM) and >600-fold selectivity over hSGLT-6. No relevant inhibition of GLUT1 is observed up to 10 μM Empagliflozin. In a kinetic binding experiments, -empagliflozin displays a high affinity for SGLT-2 with a mean Kd of 57 nM in the absence of glucose, and shows a half-life of -empagliflozin-binding to SGLT-2 of 59 min in the absence of glucose.Its binding to SGLT-2 is competitive with glucose.
    In vivo(体内研究)
    High exposure of empagliflozin is achieved in dogs, with plasma concentrations >100-fold above IC50 measured 24 h after administration of 5 mg/kg empagliflozin. The total plasma clearance of empagliflozin in ZDF rat is 43 mL/min/kg, while in dogs is lower at 1.8 mL/min/kg. Cmax of empagliflozin in ZDF rat and dogs is 167 nM and 17254 nM, respectively. Terminal elimination half-life in ZDF rat and dogs is 1.5 h and 6.3 h, respectively. Bioavailability of empagliflozin in ZDF rat is 33.2%, while in dogs is higher at 89.0%. Long-term treatment with empagliflozin, improves glycaemic controland features of metabolic syndrome in diabetic rats.
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    参考文献
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