7-Cl-O-Nec1, 受体相互作用丝氨酸/苏氨酸激酶 1 抑制剂

RIP 激酶抑制剂
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库存信息

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货号 (SKU) 包装规格 是否现货 价格 数量
N409256-1ml
1ml 现货 Stock Image
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Compound libraries (12332)

基本描述

英文别名 7-Cl-O-Nec1, Necrostatin-1 stable, Necrostatin 1S | 2,​4-​Imidazolidinedione, 5-​[(7-​chloro-​1H-​indol-​3-​yl)​methyl]​-​3-​methyl- | 5-[(7-Chloro-1H-indol-3-yl)methyl]-3-methyl-2,4-imidazolidinedione | Nec-1s | Necrostatin 2 racemate | Necrostatin 1s
规格或纯度 Moligand™, 10mM in DMSO
英文名称 7-Cl-O-Nec1
生化机理 Necrostatin 2 消旋体(Nec-1s,7-Cl-O-Nec1,Necrostatin-1 稳定型,Necrostatin 1S)是 Necrostatin-1 的稳定变体。它是一种特异性更强的 RIPK1 抑制剂,缺乏 IDO 靶向效应,对 RIPK1 的选择性是 485 种人类激酶中任何其他激酶的 1000 倍以上。
储存温度 避光,-80℃储存
运输条件 超低温冰袋运输
作用类型 抑制剂
作用机制 受体相互作用丝氨酸/苏氨酸激酶 1 抑制剂
产品介绍

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。

Information

Necrostatin 2 racemate (Nec-1s) Necrostatin 2 racemate (Nec-1s, 7-Cl-O-Nec1, Necrostatin-1 stable, Necrostatin 1S) is a stable variant of Necrostatin-1. It is a more specific RIPK1 inhibitor lacking the IDO-targeting effect, with >1000-fold more selecti
In vitro

Nec-1s is a potent inhibitor of RIPK1 and cellular necroptosis while lacking IDO inhibitory activity.

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.
Cell Data

cell lines:Cell lines:

Concentrations:

Incubation Time:

Powder Purity:≥98%

产品属性

ALogP 2.043
hba_count 2
HBD Count 2
Rotatable Bond 2

关联靶点(人)

RIPK1 Tchem 受体相互作用丝氨酸/苏氨酸蛋白激酶 1(Receptor-interacting serine/threonine-protein kinase 1) (1 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)

名称和识别符

分子类型 小分子
Canonical SMILES CN1C(=O)NC(CC2=C[NH]C3=C(Cl)C=CC=C23)C1=O
分子量 277.71
Reaxy-Rn 10175735
Reaxys-RN link address https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=10175735&ln=

化学和物理性质

敏感性 对光敏感
DMSO(mg / mL) Max Solubility 56
DMSO(mM) Max Solubility 201.65
Water(mg / mL) Max Solubility <1

安全和危险性(GHS)

Reaxy-Rn 10175735
Reaxys-RN link address https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=10175735&ln=

技术规格说明书

Concentration 9-11(mmol/L)
NMR Spectrum 1H Conforms to Structure

质检证书(CoA,COO,BSE/TSE 和分析图谱)

C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:

溶液计算器

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