CAY10746是一种选择性 Rho 激酶 (ROCK) 抑制剂,对 ROCK I 和 ROCK II 的 IC50 分别为 0.014 μM 和 0.003 μM,广泛应用于糖尿病视网膜病变(DR)等与 ROCK 信号通路相关的疾病研究。


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| 产品名称 | ROCK ↓ ↑ | ROCK1 ↓ ↑ | ROCK2 ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Thiazovivin |
+
ROCK, IC50: ~0.5 μM |
98% | |||||||||||||||||
| Netarsudil HCl |
++++
ROCK, Ki: 2 nM |
99%+ | |||||||||||||||||
| Y-33075 2HCl |
++++
ROCK, IC50: 3.6 nM |
99%+ | |||||||||||||||||
| ROCK1-IN-1 |
++
ROCK, Ki: 17nM |
95% | |||||||||||||||||
| GSK429286A |
+++
ROCK1, IC50: 14 nM |
++
ROCK2, IC50: 63 nM |
99%+ | ||||||||||||||||
| Ripasudil |
++
ROCK1, IC50: 51 nM |
++
ROCK2, IC50: 19 nM |
99%+ | ||||||||||||||||
| Belumosudil |
++
ROCK2, IC50: 60 nM ROCK2, Ki: 41 nM |
99%+ | |||||||||||||||||
| Y-27632 2HCl |
++
ROCK1, Ki: 140 nM |
+
ROCK2, Ki: 300 nM |
99%+ | ||||||||||||||||
| Fasudil HCl |
+
ROCK2, Ki: 330 nM |
PKG,Rho | 98% | ||||||||||||||||
| Chroman 1 |
++++
ROCK1, IC50: 52 pM |
++++
ROCK2, IC50: 1 pM |
99% | ||||||||||||||||
| BAY-549 |
++++
ROCK1, IC50: 0.6 nM |
++++
ROCK2, IC50: 1.1 nM |
99%+ | ||||||||||||||||
| AT13148 |
+++
ROCK1, IC50: 6 nM |
+++
ROCK2, IC50: 4 nM |
PKA | 95% | |||||||||||||||
| RKI-1447 |
+++
ROCK1, IC50: 14.5 nM |
+++
ROCK2, IC50: 6.2 nM |
99%+ | ||||||||||||||||
| Hydroxyfasudil HCl |
+
ROCK1, IC50: 0.73 μM |
+
ROCK2, IC50: 0.72 μM |
PKA | 98% | |||||||||||||||
| H-1152 2HCl |
+++
ROCK2, IC50: 0.0120 μM |
PKG | 99% | ||||||||||||||||
| GSK269962A HCl |
++++
ROCK1, IC50: 1.6 nM |
+++
ROCK2, IC50: 4 nM |
99%+ | ||||||||||||||||
| 1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 | |||||||||||||||||||
| 描述 | CAY10746 is a selective Rho kinase (ROCK) inhibitor, displaying inhibitory activity towards ROCK I and ROCK II with IC50 values of 0.014 μM and 0.003 μM, respectively, and is researched for its potential in treating diabetic retinopathy (DR) [1]. |
| 体外研究 | CAY10746 inhibits ROCK I and ROCK II, with IC50 values of 0.014 μM and 0.003 μM, respectively [1]. CAY10746, at concentrations of 0.1, 1, and 10 μM and durations of 0.25, 1, 2, and 4 hours, inhibits ROCK kinase activity in SH-SY5Y cells [1]. CAY10746 at 1 μM inhibits endothelial cell migration in vitro over periods of 24 and 36 hours [1]. CAY10746 (1 μM; 5 days) shields retinal neurons from oxidative stress and apoptosis induced by high glucose [1]. CAY10746 (1 μM; 5 days) inhibits the excessive proliferation of Müller cells and promotes the regression of vascular vessels in retinal explants exposed to a high glucose microenvironment [1]. |
| 计算器 | ||||
| 存储液制备 | ![]() |
1mg | 5mg | 10mg |
|
1 mM 5 mM 10 mM |
2.19mL 0.44mL 0.22mL |
10.93mL 2.19mL 1.09mL |
21.86mL 4.37mL 2.19mL |
|
| CAS号 | 2247240-76-0 |
| 分子式 | C26H23N3O5 |
| 分子量 | 457.48 |
| SMILES Code | O=C(NC1=CC=CC(NC(COC2=CC3=C(C=C2)C(C=CO3)=O)=O)=C1)C4=CC=C(N(C)C)C=C4 |
| 别名 | |
| 运输 | 蓝冰 |
| InChI Key | IPVJLWCNKFQWMI-UHFFFAOYSA-N |
| Pubchem ID | 156588952 |
| 存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Sealed in dry, 2-8°C |
| 溶解方案 |
DMSO: 85 mg/mL(185.8 mM),配合低频超声,并水浴加热至45℃助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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