N-[2-[2-(Dimethylamino)ethoxy]-4-(1H-pyrazol-4-yl)phenyl]-2,3-dihydro-1,4-benzodioxin-2-carboxamide

Uses

SR 3677 is an ATP-competitive inhibitor of Rho-kinases (ROCK-I/ROCK-II) which reduces amyloid-β production. It’s hypothesized that Alzheimer’s Disease, can be treated with this type of treatment, and delay further progression of the disease.

Biological Activity

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].

storage

room temperature (desiccate)

References

[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.