| 产品描述： | IPSU is a selective, orally available and brain penetrant OX2R antagonist with a pKi of 7.85. |
| 靶点： |
pKi: 7.85 (OX2R), 6.29 (OX1R);OXReceptor |
| 体外研究： |
Orexin receptor antagonists represent attractive targets for the development of drugs for the treatment of insomnia. IPSU binds rapidly and reaches equilibrium very quickly in binding and/or functional assays |
| 体内研究： |
IPSU has low blood clearance, shows high maximal blood exposure and AUC after oral dosing. It exhibits an acceptable absolute oral bioavailability and a brain/blood concentration ratio that indicated favorable brain penetration. IPSU increases sleep when dosed during the mouse active phase (lights off); IPSU induces sleep primarily by increasing NREM sleep. IPSU shows a fast onset of action, with a clear increase in total sleep time during the first hour afterdosing. The effect lasts 4-5 h, after which time the total sleep time per hour is the same as on vehicle day |
| 参考文献： |
1. Betschart C, et al. Identification of a novel series of orexin receptor antagonists with a distinct effect on sleeparchitecture for the treatment of insomnia. J Med Chem. 2013 Oct 10;56(19):7590-607. 2. Callander GE, et al. Kinetic properties of 'dual' orexin receptor antagonists at OX1R and OX2R orexin receptors. Front Neurosci. 2013 Dec 3;7:230. 3. Hoyer D, et al. Distinct effects of IPSU and suvorexant on mouse sleep architecture. Front Neurosci. 2013 Dec 10;7:235. |
| 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 |
2.466 ml |
12.331 ml |
24.661 ml |
| 5 mM |
0.493 ml |
2.466 ml |
4.932 ml |
| 10 mM |
0.247 ml |
1.233 ml |
2.466 ml |
| 50 mM |
0.049 ml |
0.247 ml |
0.493 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