• 生物活性

靶点及简介 ：Necrostatin 2 racemate 是高活性的坏死性凋亡抑制剂，为有效的 RIPK1 抑制剂，缺乏 IDO 靶向作用。

Necrostatin 2 racemate (Nec-1s, 7-Cl-O-Nec1, Necrostatin-1 stable, Necrostatin 1S)是Necrostatin-1的一种稳态变体（stable variant）,它是一种更为特异的RIPK1抑制剂，没有靶向IDO的效果，对RIPK1的选择性比对其他485种人源激酶高1000倍以上。

Necrostatin-2 racemate (also known as 7-Cl-O-Nec-1 and Nec-1s) is a potent and specific receptor-interacting protein kinase 1 (RIPK1) inhibitor lacking the IDO-targeting effect, with >1000-fold more selective for RIPK1 than for any other kinase out of 485 human kinases.

In vivo, Nec-1s is effective in reducing brain injuries. It is a superior inhibitor suitable for use in vivo lacking a paradoxical sensitizing effect in TNF-induced lethality. Nec-1s possesses several advantageous pharmacokinetic and pharmacodynamic characteristics in comparison to Nec-1. Safety profile of Nec-1s is also superior to that of Nec-1 for reduced in vivo and in vitro toxicity.

• 验证及参考文献

验证：

参考文献：

[1]. Teng X, Keys H, Jeevanandam A, Structure-activity relationship study of [1,2,3]thiadiazole necroptosis inhibitors. Bioorg Med Chem Lett. 2007 Dec 15;17(24):6836-40.

[2]. Jagtap PG, Degterev A, Choi S, Structure-activity relationship study of tricyclic necroptosis inhibitors. J Med Chem. 2007 Apr 19;50(8):1886-95.

[3]. Teng X, Degterev A, Jagtap P, Structure-activity relationship study of novel necroptosis inhibitors. Bioorg Med Chem Lett. 2005 Nov 15;15(22):5039-44.

• 溶解度及制备方案
  

  DMSO	56 mg/mL(201.65 mM)
  Water	Insoluble
  Ethanol	56 mg/mL(201.65 mM)

  Preparing Stock Solutions

Concentration/Volume/Mass	1 mg	5 mg	10 mg
1 mM	3.6009 mL	18.0044 mL	36.0088 mL
5 mM	0.7202 mL	3.6009 mL	7.2018 mL
10 mM	0.3601 mL	1.8004 mL	3.6009 mL
50 mM	0.0720 mL	0.3601 mL	0.7202 mL



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