SR-3677


CAS No. : 1072959-67-1

SR-3677,1072959-67-1
Product Details
For research use only. Not Intended for Therapeutic Use!
Cat No:I000336
Synonyms:N-[2-[2-(dimethylamino)ethoxy]-4-(1H-pyrazol-4-yl)phenyl]-2,3-dihydro-1,4-benzodioxine-3-carboxamide
Molecular Formula:C22H24N4O4
Molecular Weight:408.5
Target:ROCK
IC50:3 nM [1]
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Assay:≥95%
Appearance:A crystalline solid
Cat No:I000336
Cas No:1072959-67-1
Product-Name:SR-3677
InChIKey:OQWZIAVXCYIZNN-UHFFFAOYSA-N

SR-3677 is a new potent and selective ROCK-II inhibitor with an IC50 of ~3 nM in enzyme and cell based assays; IC50 for ROCK-I is 56 ± 12 nM.
IC50 Value: 3 nM [1]
Target: ROCK-II
in vitro: SR-3677 had an IC50 of ~3 nM in enzyme and cell based assays and had an off-target hit rate of 1.4% against 353 kinases, and inhibited only 3 out of 70 nonkinase enzymes and receptors. Pharmacology studies showed that SR-3677 was efficacious in both, increasing ex vivo aqueous humor outflow in porcine eyes and inhibiting myosin light chain phosphorylation. SR-3677 inhibited only three adrenergic receptors: α1a, α1b, and α2a with 53%, 68%, and 76% inhibition, respectively, at 3 M inhibitor concentration, which indicates IC50 values in the 1 M range or ~300 times higher than the IC50 against ROCK-II in cell-based assays [1].
in vivo: Continuous exposure of 25 M SR-3677 increases the outflow facility by 60% at 1 h perfusion, increasing to 70-80% for the 2-5 h time points (p < 0.01). This 70-80% increase in outflow is the maximal response that can be attained and is achieved at doses 2-4-fold lower than needed for Y-27632, a well studied ROCK inhibitor.TM tissue derived from the eyes perfused with 25 M SR-3677 shows a very faint band for p-MLC suggesting greater than 90% inhibition of Rho kinase in the TM tissue at this dose [1].


[1]. Feng Y, et al. 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.

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