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  • Alogliptin
    • SYR-322;阿格列汀
    货号: abs813470
    CAS号: 850649-61-5
    分子式: C18H21N5O2
    分子量: 339.39
    产品说明书
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    货号-规格 货期 价格 数量
    abs813470-5mg 1-2周 ¥1261.00
    - +
    abs813470-10mg 1-2周 ¥2309.00
    - +
    abs813470-20mg 1-2周 ¥3925.00
    - +
    大包装询价
    产品描述
    描述

    Alogliptin是一种有效的,选择性的DPP-4抑制剂,IC50为<10 nM,比作用于DPP-8和DPP-9选择性高10000倍以上。Alogliptin(SYR-322)是一种强有效的DPP-4抑制剂,比其它非常相近的丝氨酸蛋白酶DPP-8和DPP-9的选择性高出10,000倍。Alogliptin 不会抑制CYP-450 酶活性并且直到30μM浓度也不会阻断hERG 通道。

    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
    SYR-322;阿格列汀
    可溶性/溶解性
    DMSO :68 mg/mL (200.35 mM)

    Water :2 mg/mL (5.89 mM)
    生物活性
    靶点
    DPP-4
    In vitro(体外研究)
    Alogliptin is a potent (IC50 .Compound 10 is not an inhibitor of CYP-450 enzymes and does not block the hERG channel at concentrations up to 30μM.
    In vivo(体内研究)
    Absolute oral bioavailability of alogliptin in rats, dogs, and monkeys is 45%, 86%, and 72% to 88%, respectively. After a single oral dose of alogliptin, plasma DPP-4 inhibition is observed within 15 min and maximum inhibition is > 90% in rats, dogs, and monkeys; inhibition is sustained for 12 h in rats (43%) and dogs (65%) and 24 h in monkeys (> 80%). From Emax modeling, 50% inhibition of DPP-4 activity is observed at a mean alogliptin plasma concentration (EC50) of 3.4 to 5.6 ng/ml (10.0 to 16.5 nM) in rats, dogs, and monkeys. In Zucker fa/fa rats, a single dose of alogliptin (0.3, 1, 3, and 10 mg/kg) inhibites plasma DPP-4 (91% to 100% at 2 h and 20% to 66% at 24 h), increases plasma GLP-1 (2- to 3-fold increase in AUC0–20 min) and increases early-phase insulin secretion (1.5- to 2.6-fold increase in AUC0-20 min) and reduces blood glucose excursion (31%–67% decrease in AUC0–90 min) after oral glucose challenge. Alogliptin (30 and 100 mg/kg) has no effect on fasting plasma glucose in normoglycemic rats..
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