SR-3677是ROCK-II抑制剂，IC50为3 nM，对ROCK-I的IC50为56 nM。
In 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. 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.
| 分子量 | 408.45 |
| 分子式 | C22H24N4O4 |
| CAS号 | 1072959-67-1 |
| 溶解性（25°C） | 10mM in DMSO |
| 储存条件 |
粉末型式 -20°C 3年；4°C 2年 溶于溶剂 -80°C 6个月；-20°C 1个月 |
| 运输方式 | 冰袋运输，根据产品的不同，可能会有相应调整。 |
*下述溶液配置方法仅为基于分子量计算出的理论值。不同产品在配置溶液前，需考虑其在不同溶剂中的溶解度限制。
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.4483 mL | 12.2414 mL | 24.4828 mL |
| 5 mM | 0.4897 mL | 2.4483 mL | 4.8966 mL |
| 10 mM | 0.2448 mL | 1.2241 mL | 2.4483 mL |
| 小鼠 | 大鼠 | 兔 | 豚鼠 | 仓鼠 | 狗 | |
| 重量 (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| 体表面积 (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km 系数 | 3 | 6 | 12 | 8 | 5 | 20 |
| 动物 A (mg/kg) = 动物 B (mg/kg) × | 动物 B的Km系数 |
| 动物 A的Km系数 |
例如，依据体表面积折算法，将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量，需要将20 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到化合物用于大鼠的等效剂量为10 mg/kg。
| 其他相关的ROCK产品 |
|---|
| Akt/ROCK-IN-1
Akt/ROCK-IN-1 (B12) 是 Akt 和 ROCK 的双重抑制剂，IC50 分别为 0.023 nM 和 1.47 nM。 |
| Scaff10-8
Scaff10-8与RhoA结合，抑制了AKAP-Lbc-mediatedRhoA介导的RhoA活化。 |
| ROCK-IN-6
ROCK-IN-6 是一种有效的 ROCK2 抑制剂，IC50 为 2.19 nM。 |
| ROCK-IN-4
ROCK-IN-4 是一种有效的 ROCK 抑制剂，能够维持 NO 释放能力。 |
| ROCK-IN-32
ROCK-IN-32 是一种 ROCK 抑制剂，其对 ROCK2 的 IC50 值为 11 nM。 |
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