产品说明书

RIPA-56

Print
Chemical Structure| 1956370-21-0 同义名 : -
CAS号 : 1956370-21-0
货号 : A723747
分子式 : C13H19NO2
纯度 : 99%+
分子量 : 221.296
MDL号 : MFCD30738006
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
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：
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].
实验方案
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
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