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Y-27632二盐酸盐
产品纠错
CAS号:146986-50-7 | 英文名称:Y-27632 DIHYDROCHLORIDE
分子式 C14H21N3O
分子量 247
EINECS号 1312995-182-4
MDL MFCD03490488
Smiles
InChIKey
乙二醇化学百科
基本信息
中文名称 Y-27632二盐酸盐
英文名称 Y-27632 DIHYDROCHLORIDE
CAS号 146986-50-7
分子式 C14H21N3O
分子量 247.34
EINECS号 1312995-182-4
物化性质
熔点 >260°C (dec.)
沸点 462.6±15.0 °C(Predicted)
密度 1.136±0.06 g/cm3(Predicted)
溶解度 H2O: 14 mg/mL
形态 固体
酸度系数(pKa) 13.53±0.40(Predicted)
颜色 白色
稳定性 吸湿性
安全信息
危险品标志 Xn
危险类别码 20/21/22
安全说明 36
WGK Germany 3
生产及用途
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。

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)

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.

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).

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