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RIPA-56 {[allProObj[0].p_purity_real_show]}

货号:A723747

RIPA-56 is a RIP1 inhibitor with EC50 value of 28nM. It efficiently reduced TNFα-induced mortality and multi-organ damage.

RIPA-56 化学结构 CAS号:1956370-21-0
RIPA-56 化学结构
CAS号:1956370-21-0
RIPA-56 3D分子结构
CAS号:1956370-21-0
RIPA-56 化学结构 CAS号:1956370-21-0
RIPA-56 3D分子结构 CAS号:1956370-21-0
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RIPA-56 纯度/质量文件 产品仅供科研

货号:A723747 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 NF-κB 其他靶点 纯度
PDTC ammonium 98%
QNZ ++++

NF-κB, IC50: 11 nM

99%+
Sodium 4-Aminosalicylate Dihydrate 98%
Sodium Salicylate 95%
Parthenolide p53 97% HPLC
JSH-23 +

NF-κB, IC50: 7.1 μM

98%
Phenethyl caffeate 98%
Andrographolide 98+%
Curcumin Nrf2,HDAC 98%
SC75741 +++

NF-κB, EC50: 200 nM

99%+
CBL0137 HCl ++

NF-κB, EC50: 0.47 μM

p53 99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

RIPA-56 生物活性

描述 Three important signaling proteins, receptor-interacting protein 1 (RIP1), receptor-interacting protein 3 (RIP3), and mixed lineage kinase domain-like protein (MLKL), have been recognized as critical components in the regulated necrotic cell death pathway. RIPA-56 is a highly selective, potent, and metabolically stable RIP1 inhibitor with an IC50 of 13 nM. Notably, RIPA-56 had a half-life of 128 min in human liver microsomal stability assays and an EC50 of 28 nM in TSZ-induced HT-29 necrosis assay. It also demonstrated potency in protection of murine L929 cells from TZ-induced necrosis (EC50 = 27 nM). In C57BL/6 mice, both multiple-dose (0.1, 1, 3 mg/kg body weight (BW), IP, 17 min before mTNFα injection and once every 12 h) and single-dose (6 mg/kg BW, IP, 17 min before mTNFα injection) of RIPA-56 treatment dramatically increased the survival rate of TNFα-treated mice, showing a dose-dependent effect. Mice treated with multiple-dose of RIPA-56 (3 mg/kg) or a single 6 mg/kg dose of RIPA-56 had a survival rate of 100%, much higher than the TNFα/1 group, which had a survival rate of 60%[1].
作用机制 An allosteric back-pocket is isolated from RIP1 ATP binding site and forms an L-shaped hydrophobic pocket. RIPA-56 fits tightly in this pocket[1].

RIPA-56 参考文献

[1]Ren Y, Su Y, Sun L, et al. Discovery of a Highly Potent, Selective, and Metabolically Stable Inhibitor of Receptor-Interacting Protein 1 (RIP1) for the Treatment of Systemic Inflammatory Response Syndrome. J Med Chem. 2017;60(3):972-986

RIPA-56 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

4.52mL

0.90mL

0.45mL

22.59mL

4.52mL

2.26mL

45.19mL

9.04mL

4.52mL

RIPA-56 技术信息

CAS号1956370-21-0
分子式C13H19NO2
分子量 221.296
别名
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,2-8°C

溶解度

DMSO: 105 mg/mL(474.48 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方
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