S85054 |
NS6180 |
| 源叶(MedMol) | 98% |
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- 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： -20℃
- 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。
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)
