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  • MRS 2578

    • MRS-2578;MRS2578
    货号: abs813735
    CAS号: 711019-86-2
    分子式: C20H20N6S4
    分子量: 472.67
    产品说明书
    分享:
    货号-规格 货期 价格 数量
    abs813735-10mg 1-2周 ¥582.00
    - +
    abs813735-25mg 1-2周 ¥1237.00
    - +
    abs813735-50mg 1-2周 ¥2098.00
    - +
    abs813735-100mg 1-2周 ¥3776.00
    - +
    大包装询价
    产品描述
    描述

    MRS 2578是一种有效的P2Y6受体抑制剂,IC50为37 nM,对P2Y1, P2Y2, P2Y4和P2Y11受体的作用活性很弱。MRS2578 选择性阻断P2Y6受体活性,而不影响P2Y1, P2Y2, P2Y4或P2Y11 受体。在1321N1星形细胞瘤细胞中MRS2578 (1 μM) 可以完全阻断UDP对TNFalpha诱导的细胞凋亡的保护作用。 在转染有0.25 μg NF-κB启动子报告基因的HMEC-1细胞中,MRS 2578抑制 本底的NF-κB 活性并具有时间和剂量依赖特性。

    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
    MRS-2578;MRS2578
    外观
    白色粉末
    可溶性/溶解性
    DMSO :23.6 mg/mL (50 mM)
    生物活性
    靶点
    P2Y6
    In vitro(体外研究)
    MRS2578 selectively blocks P2Y6 receptor activity versus activity at P2Y1, P2Y2, P2Y4 or P2Y11 receptors. MRS2578 (1 μM) completely blocks the protection by UDP undergoing TNFalpha-induced apoptosis in 1321N1 astrocytoma cells. MRS 2578 inhibits basal NF-κB activity in time and dose dependent manner in HMEC-1 cells transfected with 0.25 μg NF-κB promoter reporter. MRS 2578 (10 μM) completely abolishes TNF-α induced NF-κB reporter activity in HMEC-1 cells. MRS 2578 (10 μM) significant reduces TNF-α–induced proinflammatory gene expression in HMEC-1 cells. MRS 2578 potentiates ATPγS and UDP response at concentrations below 316 nM whereas above this concentration, MRS 2578 inhibits ATPS- and UDP-induced IP accumulation in neonatal rat cardiac myofibroblasts. MRS2578-treated mice shows reduced bronchial hyperresponsiveness toward methacholine in OVA-sensitized mice. MRS2578 completely blocks UDP-induced the release of IL-6, KC, and IL-8 in lung epithelial cells.
    In vivo(体内研究)
    MRS 2578 (10 μM) attenuates Keratinocyte-derived chemokine serum protein levels in LPS-induced vascular inflammation in C57BL/6 mice. MRS2578 (10 μM, intratracheally) reduces BALF eosinophilia and the levels of IL-5 and IL-13 in the BALF in OVA-sensitized mice and leads to a markedly attenuated change in methacholine responsiveness after OVA challenge. MRS2578 (10 μM, intratracheally) inhibits house dust mite–induced allergic airway inflammation in OVA-sensitized mice. MRS2578 (10 μM, intratracheally) reduces of IL-6 and KC levels in BALF in OVA-sensitized mice.
    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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