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  • Anagliptin

    • SK-0403
    货号: abs811355
    CAS号: 739366-20-2
    分子式: C19H25N7O2
    分子量: 383.45
    产品说明书
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    货号-规格 货期 价格 数量
    abs811355-5mg 1-2周 ¥1689.00
    - +
    abs811355-10mg 1-2周 ¥2911.00
    - +
    大包装询价
    产品描述
    描述

    Anagliptin is a pharmaceutical drug for the treatment of type 2 diabetes mellitus.

    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
    SK-0403
    可溶性/溶解性
    DMSO: ≥ 36 mg/mL
    生物活性
    靶点
    Dipeptidyl Peptidase
    In vitro(体外研究)
    Anagliptin is a highly selective, potent inhibitor of DPP-IV, with an IC50 of 3.8 nM, and less selective at DPP-8/9 (68, 60 nM, respectively). Anagliptin does not affect CYP3A4, CYP2C19, CYP2C9, CYP1A2, and CYP2D6 (IC50 >10 μM) or CYP3A4, CYP2C8, CYP2C9, and CYP1A2 at 50 μM. Anagliptin hydrochloride does not bind to the hERG channel (E-4031, >90% inhibition at 0.1 μM, IC50 >500 μM in patch clamp using HEK 293 cells). Anagliptin (1-100 μM) dose-dependently suppresses-DPP-4-induced smooth muscle cells (SMCs) proliferation, and reduces TNF-α production in cultured monocytes.
    In vivo(体内研究)
    Anagliptin (0.3%) alters the quantity and quality of atherosclerotic lesions in apoE-deficient mice, and reduces DPP-4 activity in the plasma, and total cholesterol level, especially VLDL and LDL-C in mice. Anagliptin also decreases α-SMA-positive area and TNF-α-positive lesions in plaque area of apoE-deficient mice. In addition, Anagliptin does not increase the number of circulating endothelial progenitor cells (EPCs) in apoE-deficient mice. Anagliptin (0.3%) decreases the low-density lipoprotein cholesterol and very low-density lipoprotein cholesterol, and also reduces the sterol regulatory element-binding protein-2 messenger ribonucleic acid expression level in mice.
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