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编 号:F563395
分子式:C29H31ClN8O5
分子量:607.06
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生物活性:
GSK269962A hydrochloride (GSK 269962 hydrochloride) is a potent ROCK inhibitor with IC50s of 1.6 and 4 nM for recombinant human ROCK1 and ROCK2 respectively. GSK269962A hydrochloride has anti-inflammatory and vasodilatory activities.

体内研究:
GSK269962A is a potent antihypertensive agent. GSK269962A (0.3, 1, and 3 mg/kg; oral gavage) induces a dose-dependent reduction in blood pressure in spontaneously hypertensive rat (SHR). The reduction of blood pressure is acute and substantial.Animal Model:Male Sprague-Dawley rats (350-400g)
Dosage:0.3, 1, and 3 mg/kg
Administration:Oral gavage; 12 hours
Result:Induced a dose-dependent reduction in blood pressure.

体外研究:
GSK269962A has an IC50 of 1.6 nM toward recombinant human ROCK1. GSK269962A 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.
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