产品描述: | Belumosudil (KD025) is a selective inhibitor of ROCK2 with IC50s of 105 nM and 24 µM for ROCK2 and ROCK1, respectively. Anti-fibrotic properties |
靶点: |
ROCK2:105 nM (IC50);ROCK1:24 μM (IC50);ROCK |
体内研究: |
Belumosudil (KD-025; 100, 200 or 300 mg/kg, i.p.) dose-dependently reduces infarct volume after transient middle cerebral artery occlusion. Belumosudil is at least as efficacious in aged, diabetic or female mice, as in normal adult males |
参考文献: |
1. Boerma, M., et al. Comparative gene expression profiling in three primary human cell lines after treatment with a novel inhibitor of Rho kinase. Blood Coagul Fibrinolysis. 2008 Oct;19(7):709-18. 2. Lee, J.H., et al. Selective ROCK2 Inhibition In Focal Cerebral Ischemia. Ann Clin Transl Neurol. 2014 Jan 1;1(1):2-14. |
溶解性: |
DMSO : 250 mg/mL (552.47 mM; Need ultrasonic) H2O : < 0.1 mg/mL (insoluble) |
保存条件: |
-20℃ |
配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
1 mM |
2.21 ml |
11.049 ml |
22.099 ml |
5 mM |
0.442 ml |
2.21 ml |
4.42 ml |
10 mM |
0.221 ml |
1.105 ml |
2.21 ml |
50 mM |
0.044 ml |
0.221 ml |
0.442 ml |
|
注意: |
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