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
| 中文名称 | 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 |
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| 中文同义词 | 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;ROCK-II抑制剂(SR-3677);化合物SR-3677 |
| 英文名称 | N-[2-[2-(Dimethylamino)ethoxy]-4-(1H-pyrazol-4-yl)phenyl]-2,3-dihydro-1,4-benzodioxin-2-carboxamide |
| 英文同义词 | SR3677;N-[2-[2-(Dimethylamino)ethoxy]-4-(1H-pyrazol-4-yl)phenyl-2,3-dihydro-1,4-benzodioxin-2-carboxamidehydrochloride;SR 3677 hydrochloride;N-(2-(2-(diMethylaMino)ethoxy)-4-(1H-pyrazol-4-yl)phenyl)-2,3-dihydrobenzo[b][1,4]dioxine-2-carboxaMide;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-benzo[b][1,4]dioxin-2-carboxamide;N-[2-[2-(Dimethylamino)ethoxy]-4-(1H-pyrazol-4-yl)phenyl]-2,3-dihydro-1,4-benzodioxin-2-carboxamide |
| CAS号 | 1072959-67-1 |
| 分子式 | C22H24N4O4 |
| 分子量 | 408.45 |
| EINECS号 | |
| 相关类别 | 细胞生物学试剂 |
| Mol文件 | 1072959-67-1.mol |
| 结构式 | ![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 结构式](CAS2/GIF/1072959-67-1.gif) |
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 性质
| 沸点 | 646.9±55.0 °C(Predicted) |
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| 密度 | 1.298 |
| 储存条件 | Desiccate at RT |
| 溶解度 | DMSO：可溶15mg/mL，澄清 |
| 酸度系数(pKa) | 11.90±0.70(Predicted) |
| 形态 | 粉末 |
| 颜色 | 白色至浅棕色 |
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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.
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/04/30 | HY-13300 | SR-3677 | 5 mg | 600元 | |
| 2024/04/30 | HY-13300 | 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 SR-3677 | 1072959-67-1 | 10mM * 1mLin DMSO | 660元 |