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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, Ki: 41 nM ROCK2, IC50: 60 nM |
99%+ | |||||||||||||||||
| Y-27632 2HCl |
++
ROCK1, Ki: 140 nM |
+
ROCK2, Ki: 300 nM |
99%+ | ||||||||||||||||
| Fasudil HCl |
+
ROCK2, Ki: 330 nM |
Rho,PKG | 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 | Y-27632 is a specific inhibitor of Rho-associated kinases[1]. 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 can inhibit ROCK1 and ROCK2 in an ATP-competition manner.[1] |
| Concentration | Treated Time | Description | References | |
| ARPE19 cells | 40µM | 24 h | Y-27632 treatment significantly increased nanotube formation and mitochondrial transfer rate | Theranostics. 2024 Sep 9;14(15):5762-5777. |
| ARPE19 cells | 10µM | 24 h | Y-27632 treatment led to an increase in nanotube formation and enhanced mitochondrial transfer among ARPE19 cells | Theranostics. 2024 Sep 9;14(15):5762-5777. |
| Administration | Dosage | Frequency | Description | References | ||
| New Zealand white rabbits | Glaucoma model | Topical instillation | 2% w/v, 50 μL | Single dose, lasting for 10 days | To evaluate the therapeutic effect of HMCNs on glaucoma, results showed that HMCNs with a 20 nm shell thickness effectively reduced intraocular pressure and repaired damaged cornea and retina. | Theranostics. 2021 Mar 13;11(11):5447-5463 |
| Mice | OVA sensitised and RSV infected mouse model | Oral gavage | 30 mg/kg | Administered 2 hours before methacholine challenge | Y-27632 significantly reduced baseline lung resistance in OVA sensitised mice and suppressed methacholine and serotonin induced airway hyperresponsiveness in both OVA sensitised and OVA/RSV mice | Thorax. 2002 Jun;57(6):524-7 |
| Dose | Mice: 1 mg/kg - 5 mg/kg[8] (i.p.), 50 mg/kg[7] (i.p.) Rat: 30 mg/kg[9] (i.p.) |
| Administration | i.p. |
| 计算器 | ||||
| 存储液制备 | ![]() |
1mg | 5mg | 10mg |
|
1 mM 5 mM 10 mM |
4.04mL 0.81mL 0.40mL |
20.22mL 4.04mL 2.02mL |
40.43mL 8.09mL 4.04mL |
|
| CAS号 | 146986-50-7 |
| 分子式 | C14H21N3O |
| 分子量 | 247.34 |
| SMILES Code | O=C([C@H]1CC[C@H]([C@H](N)C)CC1)NC2=CC=NC=C2 |
| MDL No. | MFCD03093855 |
| 别名 | |
| 运输 | 蓝冰 |
| InChI Key | IDDDVXIUIXWAGJ-DDSAHXNVSA-N |
| Pubchem ID | 9901617 |
| 存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Keep in dark place, sealed in dry, 2-8°C |
| 溶解方案 |
DMSO: 25 mg/mL(101.08 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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