| 产品描述： | RIP 激酶抑制剂;RIP kinase Inhibitors;;InformationRIPA-56 RIPA-56 is a highly-potent, selective, and metabolically stable RIP1 (RIPK1) inhibitor.TargetsRIP1 (Cell-free) 13 nMIn vitroRIPA-56 shows efficient inhibition of RIP1 kinase activity, with an IC50 of 13 nM. It showed no inhibition of RIP3 kinase activity at a 10 µM concentration. RIPA-56 does not inhibit IDO activity at a concentration of 200 µM, which represents an estimated 10,000-fold selectivity window based on the RIP1 ADP-Glo activity of 13 nM.In vivoRIPA-56 has an impressive PK profile in mice, with a 3.1 h half-life, 22% oral bioavailability (PO), and 100% bioavailability from intraperitoneal injection (IP). RIPA-56 has great ability in transporting across blood brain barrier. In the SIRS mice disease model, RIPA-56 efficiently reduced tumor necrosis factor alpha (TNFα)-induced mortality and multi-organ damage. |
| 靶点： |
IC50: 13 nM (RIP1) |
| 体内研究： |
在 SIRS 小鼠疾病模型中，RIPA-56 可有效降低肿瘤坏死因子 α (TNFα) 诱导的死亡率和多器官损伤。与已知的 RIP1 抑制剂相比，RIPA-56 在人和鼠细胞中均有效，在体内更稳定，并且在动物模型研究中有效。RIPA-56 在小鼠中具有令人印象深刻的 PK 特征，半衰期为 3.1 小时，口服生物利用度 (PO) 为 22%，腹腔注射 (IP) 生物利用度为 100%。 |
| 参考文献： |
1. Ren Y, et al. Discovery of a Highly Potent, Selective, and Metabolically Stable Inhibitor of Receptor-InteractingProtein 1 (RIP1) for the Treatment of Systemic Inflammatory Response Syndrome. J Med Chem. 2017 Feb 9;60(3):972-986. |
| 保存条件： |
-80℃（运输条件：冰袋低温运输） |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
4.519 ml |
22.594 ml |
45.188 ml |
| 5 mM |
0.904 ml |
4.519 ml |
9.038 ml |
| 10 mM |
0.452 ml |
2.259 ml |
4.519 ml |
| 50 mM |
0.09 ml |
0.452 ml |
0.904 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京