Y-27632 dihydrochloride_Y-27632_Cell Cycle_ROCK_CAS号129830-38-2说明书_AbMole中国

分子量320.26
溶解性（25°C）
DMSO 64 mg/mL
分子式C H N O.2HCl Water 64 mg/mL
CAS号129830-38-2Ethanol <1 mg/mL
储存条件3年 -20°C 粉末状
生物活性
Y-27632 2HCl是一种选择性的ROCK1(p160ROCK)抑制剂，K为140 nM，比对其他激酶包括PKC，cAMP依赖性蛋白激酶， MLCK和PAK的作用强200多倍。

Y-27632也同等有效抑制ROCK-II。

Y-27632作用于PKC, cAMP依赖的蛋白激酶和肌球蛋白轻链激酶(MLCK)几乎没有活性，K分别为26 μM, 25 μM, 和 > 250 μM。

Y-27632通过选择性抑制Ca敏感化，而抑制多种兴奋剂而不是KCl，包括Phenylephrine, Histamine, Acetylcholine, Serotonin, Endothelin,和Thromboxane诱导的平滑肌收缩，IC50为0.3-1 μM。

实验操作来自于公开的文献，仅供参考
细胞实验
细胞系cyES cells
方法For 5-bromo-2′-deoxyuridine (BrdU) incorporation assays, dissociated cyES cells were seeded at a concentration of 500 cells/cm2 onto fresh feeder layers in the presence of the ROCK inhibitors Y-27632 (Wako Pure Chemical Industries, Tokyo, Japan) or Fasudil
(Tocris Bioscience, MO, USA) during the first 24 h of culture. The BrdU incorporation assay was performed using colorimetric BrdU
Cell proliferation Kit (Roche Diagnostics) according to the manufacturer's instructions. BrdU incorporations were also observed by
immunocytochemical (ICC) staining with BrdU Labeling and Detection Kit I (Roche Diagnostics).
浓度0, 0.1, 0.5, 5, 10, 20µM
处理时间24 h
动物实验
动物模型EAC modeling
配制dissolved in 0.9% NaCl
剂量0.1, 1, 10 mg/kg/day for 14 days
给药处理i.p.
不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）
小鼠大鼠兔豚鼠仓鼠狗
重量 (kg)0.020.15 1.80.40.0810
体表面积 (m)0.0070.0250.150.050.020.5
K系数36128520
动物 A (mg/kg) = 动物 B (mg/kg) ×
动物 B的K系数
动物 A的K系数
例如，依据体表面积折算法，将白藜芦醇用于小鼠的剂量22.4 mg/kg 换算成大鼠的剂量，需要将22.4 mg/kg 乘以小鼠的K系数（3），再除以大鼠的K系数（6），得到白藜芦醇用于大鼠的等效剂量为11.2 mg/kg。

参考文献
Y-27632 dihydrochloride 目录号M1817
化学数据
14213
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The ROCK inhibitor Y-27632 enhances the survival rate of human embryonic stem cells following cryopreservation. Li X, et al. Stem Cells Dev. 2008 Dec;17(6):1079-85. PMID: 19006455.
Effects of rho-associated protein kinase inhibitor Y-27632 on intraocular pressure and outflow facility.
Honjo M, et al. Invest Ophthalmol Vis Sci. 2001 Jan;42(1):137-44. PMID: 11133858.
Pharmacological properties of Y-27632, a specific inhibitor of rho-associated kinases.
Ishizaki T, et al. Mol Pharmacol. 2000 May;57(5):976-83. PMID: 10779382.。