上海莼试生物技术有限公司
上海莼试生物技术有限公司
化学性质：
| 规格 | 10mM (in 1mL DMSO) 5mg 25mg 100mg |
| CAS | 864082-47-3 |
| 别名 |
|
| 化学名 | N-(6-fluoro-1H-indazol-5-yl)-6-methyl-2-oxo-4-[4-(trifluoromethyl)phenyl]-3,4-dihydro-1H-pyridine-5-carboxamide |
| 分子式 | C21H16F4N4O2 |
| 分子量 | 432.37 |
| 溶解度 | ≥ 21.6mg/mL in DMSO, ≥ 2.73 mg/mL in EtOH with ultrasonic and warming |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice |
产品描述：
GSK429286A is a selective inhibitor of ROCK1 and ROCK2 with IC50 value of 14 nM and 63 nM, respectively [1].
Rho-kinase (ROCK) is a member of AGC (protein kinase A, protein kinase G and protein kinase C) family and plays an important role in promoting actin-myosin-mediated contractile force generation [2].
GSK429286A is a potent ROCK inhibitor and has a different activity with the reported ROCK inhibitor Y27632. Using GST method, it is shown that GSK429286A treatment (10 μM) increased MYPT phosphrylation at Thr850 via inhibiting ROCK which mediated this phosphorylation process [3].
In male Sprague-Dawley rat model with spontaneously hypertensive, oral administration of GSK429286A (30 mg/kg) marks reduced mean arterial pressure and the maximum decreased was as 50 mmHg after nearly 2 h treatment [4].
特别提醒：
1. 本产品仅供科研使用。请勿用于医药、临床诊断或治疗，食品及化妆品等用途。请勿存放于普通住宅区。
2. 为了您的安全和健康，请穿好实验服并佩戴一次性手套和口罩操作。
标签：GSK429286A
联系人：高小姐
手 机：13585831301
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