| 产品描述： | SB-649868 is a potent and selective orally active orexin (OX) 1 and OX2 receptor antagonist (pKi =9.4 and 9.5 at the OX1 and OX2 receptor, respectively). |
| 靶点： |
pKi: 9.4 (OX1), 9.5 (OX2) |
| 体外研究： |
SB-649868 is identified as one the most in vitro potent dual OX1 and OX2 receptor antagonist known at that time (pKi=9.4 and 9.5 at the OX1 and OX2 receptor, respectively) . SB-649868 antagonizes orexin-A-induced inositol 1 phosphate (IP1) accumulation with the following pKB value (OX1=9.67; OX2=9.64). SB-649868 displaces the [3H]ACT-078573 receptor binding with the following pKi values: OX1=9.27; OX2=8.91. Increasing concentrations of SB-649868 (0.3 nM-30 nM) induces a rightward shift of the orexin-A CRCs with a depression of the agonist efficacy suggesting a clear non-surmountable behavior. The calculated apparent pKb values are 9.67±0.03 and 9.64±0.07 for OX1 and OX2. |
| 参考文献： |
1. Di Fabio R, et al. Discovery process and pharmacological characterization of a novel dual orexin 1 and orexin 2receptor antagonist useful for treatment of sleep disorders. Bioorg Med Chem Lett. 2011 Sep 15;21(18):5562-7. 2. Faedo S, et al. Functional and binding kinetic studies make a distinction between OX1 and OX2 orexin receptorantagonists. Eur J Pharmacol. 2012 Oct 5;692(1-3):1-9. |
| 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 |
2.094 ml |
10.47 ml |
20.94 ml |
| 5 mM |
0.419 ml |
2.094 ml |
4.188 ml |
| 10 mM |
0.209 ml |
1.047 ml |
2.094 ml |
| 50 mM |
0.042 ml |
0.209 ml |
0.419 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