产品说明书
SAR407899
 |
同义名 : | - |
| CAS号 : | 923359-38-0 | |
| 货号 : | A303159 | |
| 分子式 : | C14H16N2O2 | |
| 纯度 : | 99%+ | |
| 分子量 : | 244.289 | |
| MDL号 : | MFCD28335199 | |
| 存储条件： |
粉末 Keep in dark place,Inert atmosphere,Room temperature 液体 -20°C:3-6个月-80°C:12个月 |
|
| 溶解度 : |
DMSO: 5 mg/mL(20.47 mM)，配合水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
|
| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | SAR407899 exhibits strong inhibitory action against ROCK by competing with ATP, showing Ki values of 36 nM for human ROCK-2 and 41 nM for rat ROCK-2. It more effectively inhibits ROCK-2 compared to ROCK-1, with inhibition concentrations (IC50s) of 102 ± 19 nM and 276 ± 26 nM, respectively, under conditions of 40 μM ATP. Moreover, SAR407899 inhibits PKC-Δ and MSK-1 with lower potency, having IC50s of 5.4 and 3.1 μM, respectively. In HeLa cells activated by PHEN, SAR407899 at concentrations of 0.1, 0.3, 1.0, and 3.0 μM selectively prevents ROCK-driven phosphorylation of MYPTT696, and demonstrates effectiveness at 1 μM and 10 μM in rat primary aortic smooth muscle cells. A concentration of 3 μM of SAR407899 fully inhibits the contraction of human umbilical vein endothelial cells (HUVECs) triggered by thrombin and formation of stress fibers. It also concentration-dependently reduces 5-bromodeoxyuridine integration into cells with an IC50 of 5.0 ± 1.3 μM and efficiently blocks THP-1 cell migration with an IC50 of 2.5 ± 1.0 μM. SAR407899 shows strong vasorelaxation effects across various isolated arteries from different species and vascular beds, with IC50 values ranging from 122 to 280 nM[1]. Furthermore, SAR407899 relaxes smooth muscle pre-contracted with phenylephrine in a dose-dependent manner, with IC50s of 0.07 and 0.05 μM[2]. | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
|
1 mM 5 mM 10 mM |
4.09mL 0.82mL 0.41mL |
20.47mL 4.09mL 2.05mL |
40.94mL 8.19mL 4.09mL |
| 参考文献 |
|---|