| 产品描述: | 产品介绍:YQ128 是有效的,选择性第二代 NLRP3 炎性体抑制剂,IC50 为 0.30 µM。YQ128 能显着和选择性地抑制 IL-1β 的产生,但不抑制 TNF-α 的产生。YQ128 可以穿过血脑屏障到达中枢神经系统。YQ128 具有抗炎活性。 |
| 体内研究: |
YQ128 (iv; 20 mg/kg) has an intermediate terminal plasma half-life (t1/2) of 6.6 hours after iv administration. YQ128 (oral; 20 mg/kg) shows delayed gastrointestinal absorption with a tmax and cmax of 12 h and 73 ng/mL, respectively. Oral bioavailability (Foral) is estimated as 10%. YQ128 exhibits extensive extravascular distribution with a large steady-state volume of distribution (Vdss) of 8.5 L/kg and rapid total clearance (CLtot) of 41 mL/min/kg. YQ128 (10 mg/kg) has been shown to trigger IL-1β production in a NLRP3- dependent manner in C57BL/6 mice. |
| 参考文献: |
1. Jiang Y, et al. Discovery of Second-Generation NLRP3 Inflammasome Inhibitors: Design, Synthesis, and Biological Characterization. J Med Chem. 2019 Oct 31. |
| 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 |
1.834 ml |
9.172 ml |
18.345 ml |
| 5 mM |
0.367 ml |
1.834 ml |
3.669 ml |
| 10 mM |
0.183 ml |
0.917 ml |
1.834 ml |
| 50 mM |
0.037 ml |
0.183 ml |
0.367 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。 |