146986-50-7

中文名称 Y-27632二盐酸盐

英文名称 Y-27632 DIHYDROCHLORIDE

CAS 146986-50-7

分子式 C14H21N3O

分子量 247.34

MOL 文件 146986-50-7.mol

更新日期 2024/05/25 10:05:26

146986-50-7 结构式

基本信息物理化学性质安全数据图谱信息常见问题列表

基本信息

中文别名

Y-27632二盐酸盐
ROCK-I和ROCK-II抑制剂
ROCK抑制剂(AZAINDOLE1)
ROCK-I和ROCK-II抑制剂(Y-27632)
反式-4-(R-1-氨基乙基)-N-(吡啶-4-基)环己烷甲酰胺
4-[(1R)-1-氨基乙基]-N-(吡啶-4-基)环己烷-1-甲酰胺
4-[(1R)-1-氨基乙基]-N-(吡啶-4-基)环己烷-1-甲酰胺二盐酸盐

英文别名

CS-20
Y-27632
Y-276322HCl
ROCK INHIBITOR
Y-27632/Y27632
Y-27632 (2HCl),98%
Y-27632, free base
Y-27632 DIHYDROCHLORIDE
Y-27632, Free Base, >99%
4-[(1R)-1-Aminoethyl]-N-(4-pyridinyl)cyclohexanecarboxamide

所属类别

生物化工：激动剂抑制剂

物理化学性质

熔点>260°C (dec.)

沸点462.6±15.0 °C(Predicted)

密度1.136±0.06 g/cm3(Predicted)

储存条件Keep in dark place,Sealed in dry,2-8°C

溶解度H₂O: 14 mg/mL

酸度系数(pKa)13.53±0.40(Predicted)

形态solid

颜色white

稳定性吸湿性

安全数据

危险性符号(GHS)

GHS07

警示词警告

危险性描述H302-H312-H332

防范说明P280

危险品标志Xn

危险类别码20/21/22

安全说明36

WGK Germany3

图谱信息

Y-27632二盐酸盐(146986-50-7)核磁图(¹HNMR)

常见问题列表

生物活性

Y-27632 是口服有效的， ATP 竞争性的 ROCK-I 和 ROCK-II 抑制剂，Ki 分别为 220 nM 和 300 nM。Y-27632 诱导凋亡 (apoptosis)。Y-27632 通过上皮-间充质过渡样调节引发人诱导多能干细胞 (hIPSCs) 选择性地分化为间胚层谱系。

靶点

ROCK-I

220 nM (Ki)

ROCK-II

300 nM (Ki)

PKN

3.1 μM (Ki)

Citron kinase

5.3 μM (Ki)

PKCα

73 μM (Ki)

PKA

25 μM (Ki)

体外研究

Y-27632 inhibits the ROCK family of kinases 100 times more potently than other kinases including protein kinase C, cAMP-dependent kinase and myosin light chain kinase. Y-27632 prolongs the lag time and delays the appearance of BrdU-labeled cells in a concentration-dependent manner, delays of about 1 and 4 h are noticed in the Swiss 3T3 cells treated with 10 and 100 μM Y-27632, respectively. Y-27632 promotes neuronal differentiation of adipose tissue-derived stem cells (ADSCs). Compared to 1.0 and 2.5 μM Y-27632 induced groups, percentages of neuroal-like cells achieved a peak in the 5.0 μM Y-27632 induced group.

体内研究

Y-27632 (5 and 10 mg/kg) significantly prolongs the onset time of myoclonic jerks when compare with saline group. Y-27632 (5 and 10 mg/kg) significantly prolongs the onset time of clonic convulsions when compare with saline group. Treatment with Dimethylnitrosamine (DMN) causes a significant decrease in rat body and liver weight (DMN-S group) compared with control animals (S-S group). Oral Y27632 (30 mg/kg) essentially prevents this DMN-induced rat body and liver weight loss (DMN-Y group).