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  • A804598

    • A 804598; A-804598
    货号: abs812003
    CAS号: 1125758-85-1
    分子式: C19H17N5
    分子量: 315.37
    产品说明书
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    货号-规格 货期 价格 数量
    abs812003-10mg 1-2周 ¥485.00
    - +
    abs812003-50mg 1-2周 ¥1455.00
    - +
    大包装询价
    产品描述
    描述

    A-804598是一个强的,竞争性,和选择性的P2X7受体拮抗剂,在大鼠,小鼠和体内的IC50分别是10 nM, 9 nM 和11 nM。

    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
    A 804598; A-804598
    可溶性/溶解性
    DMSO: ≥ 32 mg/mL
    生物活性
    靶点
    rat P2X7R ,rat P2X7R ,human P2X7R
    In vitro(体外研究)
    A-804598 represents a structurally novel, competitive, and selective antagonist that has equivalent high affinity at rat (IC50 = 10 nM), mouse (IC50 = 9 nM) and human (IC50 = 11 nM) P2X7 receptors. A-804598 also potently blocks agonist stimulated release of IL-1β(IC50 of 8.5 nM) and Yo-Pro uptake (IC50 of 8.1 nM) from differentiated THP-1 cells that natively express human P2X7 receptors. Although A-840598 potently blocks P2X7 receptor activation, at concentrations up to 100 μM, it does not significantly reduce agonist-evoked changes in intracellular calcium concentrations mediated by a variety of other P2X and P2Y receptors. A-840598 shows weak or no activity for interating with a large array of G-protein-coupled receptors, enzymes, transporters, and ion channels (CEREP, Poitiers, France)(IC50 > 5-10 μM).
    In vivo(体内研究)
    Inhibition of P2X7 through the antagonist A-804598 in SOD1-G93A mice suppresses SQSTM1/p62 up-regulation in lumbar spinal cord.
    温馨提示:本产品仅作科研实验使用,不支持临床等研究
    • 实验方法 实验条件
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