货号:A101744
同义名:
Y-27632 (hydrochloride); Y-27632 2HCl
Y-27632 dihydrochloride 是一种 ATP 竞争性的 ROCK 抑制剂,具有口服活性。Y-27632 dihydrochloride 具有一定的抗癫痫作用.


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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。 | |||||||||||||||||||
| 靶点 |
|
| 描述 | Y-27632 is a specific inhibitor of Rho-associated kinases[1]. Y-27632 2HCl is the dihydrochloride form of Y-27632 with much higher solubility than Y-27632. It is usually used for ES cell maintance[2], cell reprogramming[3],improving cell suviving after thawing[4], as well as facilitates cell proliferation and migration[5]. |
| 作用机制 | Y-27632 2HCl can inhibit ROCK1 and ROCK2 in an ATP-competition manner.[1] |
| Concentration | Treated Time | Description | References | |
| mouse airway basal stem cells | 5 mM | Maintain the stem cell morphology and characteristics of mouse airway basal stem cells, including self-renewal and airway epithelial differentiation potential | Stem Cell Res Ther. 2024 Jan 30;15(1):26. | |
| human aortic valve interstitial cells | 150 nM | 7 days | Y-27632 inhibited ROCK1 activity, reduced MYPT1 phosphorylation levels, significantly alleviated osteogenic changes in human aortic valve interstitial cells, and promoted RUNX2 ubiquitin-proteasome degradation. | Cell Death Dis. 2023 Feb 11;14(2):108. |
| Hepatic Stellate Cells | 10 μM | 3 days | Y-27632 and A-83-01 inhibited the proliferation of hepatic stellate cells and reduced the expression of α-SMA and Col1α1. | Theranostics. 2021 Mar 14;11(11):5539-5552. |
| Dose | Mice: min = 1 mg/kg[8], max = 40 mg/kg[9] Rats: min = 1 mg/kg[10], max = 100 mg/kg[9] |
| Administration | p.o., i.v., i.p. |
| 计算器 | ||||
| 存储液制备 | ![]() |
1mg | 5mg | 10mg |
|
1 mM 5 mM 10 mM |
3.12mL 0.62mL 0.31mL |
15.61mL 3.12mL 1.56mL |
31.22mL 6.24mL 3.12mL |
|
| CAS号 | 129830-38-2 |
| 分子式 | C14H23Cl2N3O |
| 分子量 | 320.26 |
| SMILES Code | O=C([C@H]1CC[C@H]([C@H](N)C)CC1)NC2=CC=NC=C2.[H]Cl.[H]Cl |
| MDL No. | MFCD03490488 |
| 别名 | Y-27632 (hydrochloride); Y-27632 2HCl |
| 运输 | 蓝冰 |
| 存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Inert atmosphere, 2-8°C |
| 溶解方案 |
DMSO: 35 mg/mL(109.29 mM),配合低频超声助溶,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 H2O: 100 mg/mL(312.25 mM),配合低频超声助溶 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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