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CAS No.: 1956370-21-0

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

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400-920-2911

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400-920-2911

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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].
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技术信息

CAS号

1956370-21-0

储存条件

分子式

C13H19NO2

运输

蓝冰

分子量

221.30

别名

溶解度

动物实验配方

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