| 产品描述： | Vipadenant (BIIB-014; CEB-4520) is an adenosine receptor antagonist, with Kis of 1.3 nM and 68 nM for A2A and A1, respectively |
| 靶点： |
Ki: 1.3 nM (A2A), 68 nM (A1), 1005 nM (A3) |
| 体内研究： |
Vipadenant (0.3-30 mg/kg) produces a dose-dependent reduction in catalepsy. Vipadenant (10 mg/kg) does not produce any statistically significant dyskinetic episodes in 6-OHDA-lesioned rats during a 19-day dosing regimen. In the mouse and rat haloperidol-induced hypolocomotion models, vipadenant has a minimum effective dose of 0.1 and 1 mg/kg, respectively. Vipadenant (3 and 10 mg/kg, p.o.) is able to increase contralateral rotations in 6-OHDA lesioned rats |
| 参考文献： |
1. Jones N, et al. A2A receptor antagonists do not induce dyskinesias in drug-naive or L-dopa sensitized rats. Brain Res Bull. 2013 Sep;98:163-9. 2. Brian C. Shook, et al. Adenosine A2A Receptor Antagonists and Parkinson’s Disease. ACS Chem Neurosci. 2011 Oct 19; 2(10): 555-567. |
| 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 |
3.112 ml |
15.56 ml |
31.12 ml |
| 5 mM |
0.622 ml |
3.112 ml |
6.224 ml |
| 10 mM |
0.311 ml |
1.556 ml |
3.112 ml |
| 50 mM |
0.062 ml |
0.311 ml |
0.622 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