| 产品描述： | AZ194 is a first-in-class, orally active inhibitor of CRMP2-Ubc9 interaction and inhibitor of NaV1.7 (IC50=1.2 μM). AZ194 blocks SUMOylation of CRMP2 to selectively reduce the amount of surface-expressed NaV1.7. Antinociceptive effects |
| 靶点： |
Sodium Channel |
| 体内研究： |
AZ194 would provide pain relief in rat models of chemotherapy- and nerve injury- induced neuropathic pain. AZ194 (orally; at 2 and 10 mg/kg) restores mechanical sensitivity in animals with chemotherapy-induced and nerve injury-induced neuropathic nociception. AZ194 (10 mg/kg; ip; CD1 male mice) does not affect motor performance (open field). AZ194 synergizes with commonly used painkillers, engages NaV1.7-dependent endogenous opioid signaling |
| 参考文献： |
1. Cai S, et al. Selective targeting of NaV1.7 via inhibition of the CRMP2-Ubc9 interaction reduces pain in rodents. Sci Transl Med. 2021;13(619):eabh1314. |
| 溶解性： |
Soluble in DMSO |
| 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 |
1.762 ml |
8.808 ml |
17.617 ml |
| 5 mM |
0.352 ml |
1.762 ml |
3.523 ml |
| 10 mM |
0.176 ml |
0.881 ml |
1.762 ml |
| 50 mM |
0.035 ml |
0.176 ml |
0.352 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