Y-27632二盐酸盐
中文名称:
Y-27632二盐酸盐
中文同义词:
4-[(1R)-1-氨基乙基]-N-(吡啶-4-基)环己烷-1-甲酰胺二盐酸盐;Y-27632二盐酸盐;ROCK抑制剂(AZAINDOLE1);ROCK-I和ROCK-II抑制剂;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
英文名称:
Y-27632 DIHYDROCHLORIDE
英文同义词:
ROCK INHIBITOR;(R)-(+)-TRANS-N-(4-PYRIDYL)-4-(1-AMINOETHYL)-CYCLOHEXANECARBOXAMIDE 2HCL;(R)-(+)-TRANS-4-(1-AMINOETHYL)-N-(4-PYRIDYL)CYCLOHEXANECARBOXAMIDE DIHYDROCHLORIDE;(+)-R-TRANS-4-(AMINOETHYL)-N-(4-PYRIDYL)-CYCLOHEXANECARBOXAMIDE 2HCL H2O;Y-27632;Y-27632 DIHYDROCHLORIDE;TRANS-4-[(1R)-1-AMINOETHYL]-N-4-PYRIDINYLCYCLOHEXANECARBOXAMIDE DIHYDROCHLORIDE;Y-276322HCl
CAS号:
146986-50-7
分子式:
C14H21N3O
分子量:
247.34
EINECS号:
1312995-182-4
相关类别:
高纯试剂;医药中间体;小分子抑制剂;小分子抑制剂，天然产物;细胞生物学试剂;Inhibitors;Protein Kinase;Signalling;Inhibitor;APIs
Mol文件:
146986-50-7.mol
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
形态
solid
酸度系数(pKa)
13.53±0.40(Predicted)
颜色
white
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)
ROCK-I
220 nM (Ki)
ROCK-II
300 nM (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).
危险品标志
Xn
危险类别码
20/21/22
安全说明
36
WGK Germany
3
