| 产品描述： | NP118809 is a potent N-type calcium channel blocker, with an IC50 of 0.11 μM; also less potently inhibits L-type calcium channel with an IC50 of 12.2 μM. |
| 靶点： |
N-type calcium channel:0.11 μM (IC50);L-type calcium channel:12.2 μM (IC50);CalciumChannel |
| 体内研究： |
NP118809 (25 mg/kg, i.p.) shows significant analgesic activity in the phase IIA portions of the rat formalin model. NP118809 (30 mg/kg, p.o.) results in 80.3% inhibition of mechanical allodynia and 96.3% inhibition of thermal hyperalgesia in the rat spinal nerve ligation model |
| 参考文献： |
1. Zamponi GW, et al. Scaffold-based design and synthesis of potent N-type calcium channel blockers. Bioorg Med Chem Lett. 2009 Nov 15;19(22):6467-72. 2. Pajouhesh H, et al. Structure-activity relationships of diphenylpiperazine N-type calcium channel inhibitors. Bioorg Med Chem Lett. 2010 Feb 15;20(4):1378-83. |
| 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 |
2.171 ml |
10.855 ml |
21.71 ml |
| 5 mM |
0.434 ml |
2.171 ml |
4.342 ml |
| 10 mM |
0.217 ml |
1.086 ml |
2.171 ml |
| 50 mM |
0.043 ml |
0.217 ml |
0.434 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