| 产品描述： | GSK429286A is a selective inhibitor of ROCK1 with an IC50 value of 14 nM. |
| 靶点： |
ROCK1:14 nM (IC50);RSK:780 nM (IC50);p70S6K:1940 nM (IC50);ROCK |
| 体内研究： |
GSK429286A has 61% oral bioavailability in male Sprague-Dawley rats. Oral administration of GSK429286A at single doses of 3-30 mg/kg dramatically reduces mean arterial pressure in the spontaneously hypertensive rats (SHRs) in a dose-dependent manner, with a maximum decrease of 50 mmHg after approximately 2 hours treatment at dose of 30 mg/kg |
| 参考文献： |
1. Goodman KB et al Development of dihydropyridone indazole amides as selective Rho-kinase inhibitors. J Med Chem. 2007 Jan 11;50(1):6-9. 2. Nichols RJ et al Substrate specificity and inhibitors of LRRK2, a protein kinase mutated in Parkinson's disease. Biochem J. 2009 Oct 23;424(1):47-60. |
| 溶解性： |
DMSO : ≥ 51 mg/mL (117.95 mM) |
| 保存条件： |
-20℃ |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.313 ml |
11.564 ml |
23.128 ml |
| 5 mM |
0.463 ml |
2.313 ml |
4.626 ml |
| 10 mM |
0.231 ml |
1.156 ml |
2.313 ml |
| 50 mM |
0.046 ml |
0.231 ml |
0.463 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