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Overview
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Background
SR-3677 is a novel, potent and highly selective inhibitor of Rho Kinase (ROCK-II) with the IC50 value of ~0.3nM in enzyme and cell based assays [1].SR-3677 has been reported to selectively inhibit the ROCK- II with the IC50 values of ~3nM, ~3nM, 56nM, 3.968μM,1.190μM and 7.491μM for ROCK-II,ppMLC, ROCK-I, PKA, MRCK and Akt1, respectively. In addition, SR-3677 has been shown several key binding elements that contribute to the high potency and selectivity in the docking assay. Furthermore, SR-3677 has been revealed to be efficacious in enhancing aqueous humor outflow and in target modulation in the pharmacology studies [1].
[1] Feng Y1, Yin Y, Weiser A, Griffin E, Cameron MD, Lin L, Ruiz C, Schürer SC, Inoue T, Rao PV, Schröter T, Lograsso P. Discovery of substituted 4-(pyrazol-4-yl)-phenylbenzodioxane-2-carboxamides as potent and highly selective Rho kinase (ROCK-II) inhibitors. J Med Chem. 2008 Nov 13;51(21):6642-5. doi: 10.1021/jm800986w. Epub 2008 Oct 4.
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- Properties
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Overview