| 產品描述： | GSK429286A is a selective inhibitor of ROCK1 with an IC50 value of 14 nM. |
| 靶點： |
ROCK1:14 nM (IC50);RSK:780 nM (IC50);p70S6K:1940 nM (IC50);ROCK |
| 體內研究： |
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 |
| 參考文獻： |
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) |
| 保存條件： |
-20℃ |
| 配置溶液濃度參考： |
|
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： |
部分產品我司僅能提供部分信息，我司不保證所提供信息的權威性，僅供客戶參考交流研究之用。 |
上海工商
危險品化學品經營許可證（不帶存儲）
營業(yè)執(zhí)照(三證合一)
北京