中文名 | SR-3677 |
英文名 | N-[2-[2-(Dimethylamino)Ethoxy]-4-(1H-Pyrazol-4-yl)Phenyl]-2,3-Dihydro-1,4-Benzodioxin-2-Carboxamide |
别名 | 化合物SR-3677 ROCK-II抑制剂(SR-3677) 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 |
英文别名 | SR3677 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 N-[2-[2-(Dimethylamino)Ethoxy]-4-(1H-Pyrazol-4-yl)Phenyl]-2,3-Dihydro-1,4-Benzodioxin-2-Carboxamide N-[2-[2-(Dimethylamino)ethoxy]-4-(1H-pyrazol-4-yl)phenyl]-2,3-dihydro-benzo[b][1,4]dioxin-2-carboxamide N-(2-(2-(diMethylaMino)ethoxy)-4-(1H-pyrazol-4-yl)phenyl)-2,3-dihydrobenzo[b][1,4]dioxine-2-carboxaMide N-[2-[2-(Dimethylamino)ethoxy]-4-(1H-pyrazol-4-yl)phenyl-2,3-dihydro-1,4-benzodioxin-2-carboxamidehydrochloride |
CAS | 1072959-67-1 |
化学式 | C22H24N4O4 |
分子量 | 408.45 |
密度 | 1.298 |
沸点 | 646.9±55.0 °C(Predicted) |
溶解度 | DMSO: 可溶15mg/mL,澄清 |
酸度系数 | 11.90±0.70(Predicted) |
存储条件 | Desiccate at RT |
外观 | 粉末 |
颜色 | white to light brown |
体外研究 | 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. |
体内研究 | 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. |
危险品标志 | Xi - 刺激性物品 |
风险术语 | 36/37/38 - 刺激眼睛、呼吸系统和皮肤。 |
安全术语 | 26 - 不慎与眼睛接触后,请立即用大量清水冲洗并征求医生意见。 |
WGK Germany | 3 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.448 ml | 12.241 ml | 24.483 ml |
5 mM | 0.49 ml | 2.448 ml | 4.897 ml |
10 mM | 0.245 ml | 1.224 ml | 2.448 ml |
5 mM | 0.049 ml | 0.245 ml | 0.49 ml |
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