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146986-50-7

中文名稱 Y-27632二鹽酸鹽
英文名稱 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 2025/02/04 21:49:07
146986-50-7 結(jié)構(gòu)式 146986-50-7 結(jié)構(gòu)式

基本信息

中文別名
Y-27632二鹽酸鹽
ROCK-I和ROCK-II抑制劑
ROCK抑制劑(AZAINDOLE1)
ROCK-I和ROCK-II抑制劑(Y-27632)
反式-4-(R-1-氨基乙基)-N-(吡啶-4-基)環(huán)己烷甲酰胺
4-[(1R)-1-氨基乙基]-N-(吡啶-4-基)環(huán)己烷-1-甲酰胺
4-[(1R)-1-氨基乙基]-N-(吡啶-4-基)環(huán)己烷-1-甲酰胺二鹽酸鹽
英文別名
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
所屬類別
生物化工:激動劑抑制劑

物理化學(xué)性質(zhì)

熔點>260°C (dec.)
沸點462.6±15.0 °C(Predicted)
密度1.136±0.06 g/cm3(Predicted)
儲存條件Keep in dark place,Sealed in dry,2-8°C
溶解度H2O: 14 mg/mL
酸度系數(shù)(pKa)13.53±0.40(Predicted)
形態(tài)solid
顏色white
穩(wěn)定性吸濕性

安全數(shù)據(jù)

危險性符號(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險性描述H302-H312-H332
防范說明P280
危險品標(biāo)志Xn
危險類別碼20/21/22
安全說明36
WGK Germany3
Y-27632二鹽酸鹽價格(試劑級)
報價日期產(chǎn)品編號產(chǎn)品名稱CAS號包裝價格
2025/02/08HY-10583Y-27632二鹽酸鹽
Y-27632 dihydrochloride
146986-50-72 mg450元
2025/02/08HY-10583Y-27632二鹽酸鹽
Y-27632 dihydrochloride
146986-50-75mg700元
2025/02/08HY-10583Y-27632二鹽酸鹽
Y-27632 dihydrochloride
146986-50-710mM * 1mLin DMSO770元

常見問題列表

生物活性
Y-27632 是口服有效的, ATP 競爭性的 ROCK-I 和 ROCK-II 抑制劑,Ki 分別為 220 nM 和 300 nM。Y-27632 誘導(dǎo)凋亡 (apoptosis)。Y-27632 通過上皮-間充質(zhì)過渡樣調(diào)節(jié)引發(fā)人誘導(dǎo)多能干細(xì)胞 (hIPSCs) 選擇性地分化為間胚層譜系。
靶點

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)

體外研究

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.

體內(nèi)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).

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