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Biological Activity:
Highly potent and selective inhibitor of Rho-Kinase (ROCK), with IC50 values: 1.6 nM toward ROCK1 and 6 nM toward ROCK2 and high kinase selectivity (>30 fold selective for ROCK compared to other protein kinases tested) and with antihypertensive activity; cardiovascular diseases category.
GSK269962A has a much improved potency and selectivity in comparison with Y-27632, which has IC50 values of 140-220 nM for ROCK1 and ROCK2.
References: online ref 1
C Doe et al. Novel Rho Kinase Inhibitors with Anti-inflammatory and Vasodilatory Activities. J. Pharmacol. Exp. Ther. 2007, 320, 89-98. [online]
D Schaafsma et al. Rho kinase inhibitors: A novel therapeutical intervention in asthma? Eur. J. Pharmacol. 2008, 585(2-3), 398-406. [online]
Chemical Name: N-(3-{[2-(4-amino-1,2,5-oxadiazol-3-yl)-1-ethyl-1H-imidazo[4, 5-c]pyridin-6-yl]oxy}phenyl)-4-{[2-(4-morpholinyl)ethyl]-oxy}benzamide
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