GSK269962A(GSK269962),850664-2

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抑制剂描述：

产品名称：GSK269962A(GSK269962)

产品别名：见爱必信官网

英文别名：GSK269962A(GSK269962)

靶点：ROCK

CAS：850664-21-0

纯度：＞98%

外观：见爱必信官网

保存方法：Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.

描述：

GSK269962A(GSK269962)是人ROCK1和ROCK2抑制剂，IC50分别为1.6和4 nM，比对其它丝氨酸/苏氨酸激酶的抑制性强30倍。

溶解性：DMSO : ≥ 30 mg/mL (52.58 mM)

体外研究：

GSK269962A IC50 values of 1.6 nM toward recombinant human ROCK1. GSK269962A also exhibits more than 30-fold selectivity against a panel of serine/threonine kinases. GSK269962A induces vasorelaxation in preconstricted rat aorta with an IC50 of 35 nM. Both are highly potent toward human ROCK1 with IC50 of 1.6 nM for GSK269962A. On the other hand, GSK269962A has a significantly improved kinase selectivity profile with at least >30-fold selectivity against the panel of protein kinase tested.

体内研究：Oral administration of GSK269965A (0.3, 1, and 3 mg/kg) induces a dose-dependent reduction in blood pressure in spontaneously hypertensive rat (SHR). The reduction of blood pressure is acute and substantial. The maximal effect on blood pressure is observed approximately 2 h after oral gavages for both compounds. Under a similar setting, oral administration of Y-27632 (10 and 30 mg/kg) also induced a dose-dependent decrease of blood pressure. For all three Rho kinase inhibitors, the reduction of blood pressure is accompanied by an acute, dose-dependent increase in heart rate, presumably due to the activation of baroreflex mechanism.

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