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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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 | ✔ | HDAC,Nrf2 | 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。 |
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]. |
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 |
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 |