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Necrostatin-1

Necrostatin-1是一种特异性的RIP1抑制剂,抑制TNF-α诱导的坏死,EC50为490 nM。

目录号
EY1500
EY1500
EY1500
EY1500
纯度
99.29%
99.29%
99.29%
99.29%
规格
5 mg
10 mg
50 mg
100 mg
原价
350
600
1200
1800
售价
350
600
1200
1800
库存
现货
现货
现货
现货
订购
订购
订购
订购
订购
订购
  • 生物活性

    In vitro: Previous study indicated that necrostatin-1 was a selective allosteric inhibitor of the death domain receptor–associated adaptor kinase RIP1 in vitro. In this study, RIP1 was found to be the primary cellular target responsible for the antinecroptosis activity of necrostatin-1. In addition, two other necrostatins, necrostatin-3 and necrostatin-5, were also shown to target the RIP1 kinase step in the necroptosis pathway, but through different mechanism compared with that of necrostatin-1. The findings established necrostatins as the first-in-class inhibitors of RIP1 kinase, the key upstream kinase involved in the activation of necroptosis. In vivo: A previous study was designed to investigate the protective effects and mechanisms of Nec-1 in concanavalin A-induced hepatitis in mice. It was found that in Nec-1-treated mice the amelioration in liver functions and histopathological changes and the suppression of inflammatory cytokine production were observed. Western blotting analyses showed that the expression of TNF-α, IFN-γ, IL2, IL6, and RIP1 was significantly reduced in the Nec-1-treated mice, which was further confirmed by immunofluorescence and immunohistochemistry. In addition, autophagosome formation was significantly reduced by Nec-1 treatment. These results indicated that Nec-1 could prevent concanavalin A -induced liver injury via RIP1-related and autophagy-related pathways.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

    0.01-100 μM

  • 动物实验

  • 不同实验动物依据体表面积的等效剂量转换表(数据来源于FDA指南)

    动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 AKm系数


    例如,已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法:将88 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到该药物用于大鼠的等效剂量44 mg/kg。


  • 参考文献

    [1] Degterev A, et al. Nat Chem Biol, 2008, 4(5), 313-321.
    [2] Degterev, A., et al. 2005. Nat. Chem. Biol. 1: 112-119.

    分子式
    C13H13N3OS
    分子量
    259.33
    CAS号
    4311-88-0
    储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂(常温)
    DMSO
    25 mg/mL
    Water
    <1 mg/mL
    Ethanol
    6 mg/mL

    体内溶解度

  • Clinical Trial Information ( data from http://clinicaltrials.gov )

    注:以上所有数据均来自公开文献,并不保证对所有实验均有效,数据仅供参考。

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