SR-3677

• CAT Number: I000336
• CAS Number: 1072959-67-1
• Molecular Formula: C22H24N4O4
• Molecular Weight: 408.5
• Purity: ≥95%
• Target: ROCK
• Solubility: DMSO: ≥ 43 mg/mL
• Storage: Store at -20C
• IC50: 3 nM [1]
• 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-IIin 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].

Reference

[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.