| 产品描述: | RIPA-56 is a highly potent, selective, and metabolically stable inhibitor of receptor-interacting protein 1 (RIP1) with an IC50 of 13 nM. RIPA-56 can be used for the treatment of systemic inflammatory response syndrome |
| 靶点: |
IC50: 13 nM (RIP1);RIPkinase |
| 体外研究: |
RIPA-56 shows efficient inhibition of RIP1 kinase activity, with an IC50 of 13 nM and no inhibition of RIP3 kinase activity at a 10 μM concentration. RIPA-56 also demonstrates potency in protection of murine L929 cells from TNFα/z-VAD-FMK (TZ)-induced necrosis (EC50=27 nM) |
| 体内研究: |
In the SIRS mice disease model, RIPA-56 efficiently reduces tumor necrosis factor alpha (TNFα)-induced mortality and multi-organ damage. Compared to known RIP1 inhibitors, RIPA-56 is potent in both human and murine cells, is much more stable in vivo, and is efficacious in animal model studies. RIPA-56 has an impressive PK profile in mice with a 3.1 h half-life, 22% oral bioavailability (P.O.), and 100% bioavailability from intraperitoneal injection (I.P.) |
| 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. |
| 溶解性: |
soluble in DMSO |
| 保存条件: |
-20℃ |
| 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。 |