1072959-67-1
1072959-67-1 结构式
基本信息
N-[2-[2-(二甲基氨基)乙氧基]-4-(1H-吡唑-4-基)苯基]-2,3-二氢-1,4-苯并二恶烷-2-甲酰胺
CS-1125
CS-2825
SR-3677
SR 3677
SR 3677 hydrochloride
SR 3677 dihydrochloride
N-(2-(2-(Dimethylamino)ethoxy)-4-(1H-pyrazol-4-yl)phenyl)-2,3-dihydrobenzo[b][1,4]dioxine-2-ca
N-[2-[2-(Dimethylamino)ethoxy]-4-(1H-pyrazol-4-yl)phenyl]-2,3-dihydro-1,4-benzodioxin-2-carboxamide
1,4-Benzodioxin-2-carboxamide, N-[2-[2-(dimethylamino)ethoxy]-4-(1H-pyrazol-4-yl)phenyl]-2,3-dihydro-
N-[2-[2-(Dimethylamino)ethoxy]-4-(1H-pyrazol-4-yl)phenyl]-2,3-dihydro-benzo[b][1,4]dioxin-2-carboxamide
物理化学性质
常见问题列表
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ROCK-II 3 nM (IC 50 ) |
ROCK-I 56 nM (IC 50 ) |
SR-3677 has an IC 50 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 IC 50 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.
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.