Y-27632|146986-50-7|-陌孚医药/Medlife

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Y-27632

目录号: PC15955 纯度: ≥99%

CAS No. :146986-50-7

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PC15955-200mg	200mg	¥6065.00	请登录
PC15955-10mM (in 1mL DMSO)	10mM (in 1mL DMSO)	¥699.00	请登录

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中文名称	Y-27632
中文别名	Y-27632二盐酸盐;4-[(1R)-1-氨基乙基]-N-(吡啶-4-基)环己烷-1-甲酰胺二盐酸盐;三(2,2,6,6-四甲基-3,5-庚二酮)鉻(Ⅲ);4-[(1R)-1-氨基乙基]-N-(吡啶-4-基)环己烷羧酰胺;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;Y-27632 二盐酸盐
英文名称	Y-27632
英文别名	Y-27632 DIHYDROCHLORIDE;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;TRANS-4-[(1R)-1-AMINOETHYL]-N-4-PYRIDINYLCYCLOHEXANECARBOXAMIDE DIHYDROCHLORIDE;Y-276322HCl;Cyclohexanecarboxamide, 4-[(1R)-1-aminoethyl]-N-4-pyridinyl-, trans-;Y27632;Y-27632;4-[(1R)-1-aminoethyl]-N-pyridin-4-ylcyclohexane-1-carboxamide;Y-27632-dihydrochloride;4-[(1R)-1-Aminoethyl]-N-pyridin-4-ylcyclohexane-1-carboxamide dihydrochloride;Y-27632, free base;4-[(1R)-1-Aminoethyl]-N-(4-pyridinyl)cyclohexanecarboxamide;Y-27632/Y27632;Y-27632 (2HCl),98%;Y-27632, Free Base, >99%
Cas No.	146986-50-7
分子式	C₁₄H₂₁N₃O
分子量	320.26
包装储存	-20°C, protect from light, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

生物活性

Y-27632 is an orally active, ATP-competitive inhibitor of ROCK-I and ROCK-II, with K_is of 220 and 300 nM, respectively. Y-27632 attenuates Doxorubicin-induced apoptosis of human cardiac stem cells. Y-27632 also suppresses dissociation-induced apoptosis of murine prostate stem/progenitor cells. Y-27632 primes human induced pluripotent stem cells (hIPSCs) to selectively differentiate towards mesendodermal lineage via epithelial-mesenchymal transition-like modulation.

性状

Solid

IC50 & Target[1][2]

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(In Vitro)

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.
Extracellular matrix (ECM) molecules decreases apoptosis markers and inhibiting the ROCK pathway blocks ECM stimulated actin cortical mat reformation and increases apoptosis in embryonic corneal epithelial cells.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

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).

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature or refrigerated transportation.

储存方式

-20°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

参考文献

[1]. Ishizaki T, et al. Pharmacological properties of Y-27632, a specific inhibitor of rho-associated kinases. Mol Pharmacol. 2000 May;57(5):976-83. [Information]

[2]. Xue ZW, et al. Rho-associated coiled kinase inhibitor Y-27632 promotes neuronal-like differentiation of adult human adipose tissue-derived stem cells.Chin Med J (Engl). 2012 Sep;125(18):3332-5. [Information]

[3]. Tada S, et al. A selective ROCK inhibitor, Y27632, prevents dimethylnitrosamine-induced hepatic fibrosis in rats. J Hepatol. 2001 Apr;34(4):529-36. [Information]

[4]. Inan S, et al. Antiepileptic effects of two Rho-kinase inhibitors, Y-27632 and fasudil, in mice. Br J Pharmacol. 2008 Sep;155(1):44-51. [Information]

[5]. Maldonado M, et al. ROCK inhibitor primes human induced pluripotent stem cells to selectively differentiate towardsmesendodermal lineage via epithelial-mesenchymal transition-like modulation. Stem Cell Res. 2016 Sep;17(2):222-227. [Information]

[6]. Kan L, et al. Rho-Associated Kinase Inhibitor (Y-27632) Attenuates Doxorubicin-Induced Apoptosis of Human Cardiac Stem Cells. PLoS One. 2015;10(12):e0144513. Published 2015 Dec 8. [Information]

[7]. Zhang L, et al. ROCK inhibitor Y-27632 suppresses dissociation-induced apoptosis of murine prostate stem/progenitor cells and increases their cloning efficiency. PLoS One. 2011;6(3):e18271. Published 2011 Mar 28. [Information]

[8]. Svoboda KK, et al. ROCK inhibitor (Y27632) increases apoptosis and disrupts the actin cortical mat in embryonic avian corneal epithelium. Dev Dyn. 2004;229(3):579-590. [Information]

溶解度数据

体外研究:

DMSO : 50 mg/mL (202.15 mM; Need ultrasonic)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	4.0430 mL	20.2151 mL	40.4302 mL
5 mM	0.8086 mL	4.0430 mL	8.0860 mL
10 mM	0.4043 mL	2.0215 mL	4.0430 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

建议依照次序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (10.11 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (10.11 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH?O 中，得到澄清透明的生理盐水溶液
2.

建议依照次序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (10.11 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (10.11 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

建议依照次序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (10.11 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (10.11 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。
4.

建议依照次序添加每种溶剂： Saline
Solubility: 2 mg/mL (8.09 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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