SR-3677 is a potent and selective ROCK-II inhibitor with an IC50 of ~3 nM.
性状
Solid
IC50 & Target[1][2]
ROCK-II
3 nM (IC50)
ROCK-I
56 nM (IC50)
体外研究(In Vitro)
SR-3677 has an IC50 of ~3 nM in enzyme and cell based assays and has an off-target hit rate of 1.4% against 353 kinases, and inhibits only 3 out of 70 nonkinase enzymes and receptors. The IC50 value of SR-3677 for ROCK-I is 56±12 nM. The hydrophobic interaction of the benzodioxane phenyl ring with the hydrophobic surface of the pocket is the dominating factor that contributes to the high potency of SR-3677.
Medlife has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
ExVivo: Pharmacology studies shows that SR-3677 is efficacious in both, increasing ex vivo
aqueous humor outflow in porcine eyes and inhibiting myosin light chain phosphorylation. Continuous exposure of 25 μM SR-3677 increases the outflow facility by 60% at 1 h perfusion, increasing to 70–80% for the 2–5 h time points.
Medlife has not independently confirmed the accuracy of these methods. They are for reference only.