| 产品描述： | NS6180 is a new orally active KCa3.1 channel inhibitor. NS6180 inhibits cloned human KCa3.1 channels with an IC50value of 9 nM. NS6180 can be used for the research of inflammatory bowel disease (IBD) |
| 靶点： |
Potassium Channel |
| 体外研究： |
NS6180 (0.001-1 μM) shows inhibition of human KCa3.1 with an IC50 value of 9.4 nM and a K50 value of 11 1.7 nM, respectively. NS6180 (30 nM, 10 μM) has inhibition that dependent on amino acid residues T250 and V275. NS6180 (1, 10, 100 and 1000 nM; 1 min) shows CCCPreported hyperpolarizations of human erythrocytes. NS6180 (1, 10, 100 and 1000 nM; 1 min) blocks the erythrocyte KCa3.1 channels with IC50 values of 14 nM (human KCa3.1 channels), 15 nM (mouse) and 9 nM (rats), respectively. NS6180 (0-5 μM, 48 h) suppresses rat and mouse splenocyte proliferation at submicrolar concentrations and potently inhibited IL-2 and IFN-g production, while exerting smaller effects on IL-4 and TNF-α and no effect on IL-17 production |
| 体内研究： |
NS6180 (i.v., i.p. and oral administration; 10 mg/kg; twice daily or once daily) has extremely low bioavailability and reduces DNBS-induced experimental colitis in rats. Animal Model: Rats Dosage: 10 mg/kg Administration: i.v., i.p. and oral administration; 10 mg/kg; twice daily or once daily Result: Had a plasma half-life of 3.8 h, oral or i.p. administration gave low plasma exposure (Cmax: 186 nM and 33 nM, respectively, after administration of 10 mg/kg). |
| 参考文献： |
1. Strobak D, et al. NS6180, a new K(Ca) 3.1 channel inhibitor prevents T-cell activation and inflammation in a rat model of inflammatory bowel disease. Br J Pharmacol. 2013 Jan;168(2):432-44. |
| 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 |
3.093 ml |
15.464 ml |
30.928 ml |
| 5 mM |
0.619 ml |
3.093 ml |
6.186 ml |
| 10 mM |
0.309 ml |
1.546 ml |
3.093 ml |
| 50 mM |
0.062 ml |
0.309 ml |
0.619 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