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Y-27632二盐酸盐 /Y-27632 dihydrochloride 99%+

货号:A101744 同义名: Y-27632 (hydrochloride);Y-27632 2HCl Ambeed 开学季,买赠积分,赢豪礼

Y-27632 dihydrochloride 是一种 ATP 竞争性的 ROCK 抑制剂,具有口服活性。Y-27632 dihydrochloride (GMP) 具有抗癫痫作用,可用于细胞研究生产的辅助试剂。

Y-27632 dihydrochloride 化学结构 CAS号:129830-38-2
Y-27632 dihydrochloride 化学结构
CAS号:129830-38-2
Y-27632 dihydrochloride 3D分子结构
CAS号:129830-38-2
Y-27632 dihydrochloride 化学结构 CAS号:129830-38-2
Y-27632 dihydrochloride 3D分子结构 CAS号:129830-38-2
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Y-27632 dihydrochloride 纯度/质量文件 产品仅供科研

货号:A101744 标准纯度: 99%+
批次查询: 批次纯度:

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产品名称 ROCK ROCK1 ROCK2 其他靶点 纯度
Thiazovivin +

ROCK, IC50: ~0.5 μM

98%
Netarsudil hydrochloride ++++

ROCK, Ki: 2 nM

99%+
Y-33075 2HCl ++++

ROCK, IC50: 3.6 nM

99%+
ROCK1-IN-1 ++

ROCK, Ki: 17nM

95%
GSK429286A +++

ROCK1, IC50: 14 nM

++

ROCK2, IC50: 63 nM

99%+
Ripasudil ++

ROCK1, IC50: 51 nM

++

ROCK2, IC50: 19 nM

99%+
Belumosudil ++

ROCK2, IC50: 60 nM

ROCK2, Ki: 41 nM

99%+
Y-27632 dihydrochloride ++

ROCK1, Ki: 140 nM

+

ROCK2, Ki: 300 nM

99%+
Fasudil HCl +

ROCK2, Ki: 330 nM

Rho,PKG 98%
Chroman 1 ++++

ROCK1, IC50: 52 pM

++++

ROCK2, IC50: 1 pM

99%
BAY-549 ++++

ROCK1, IC50: 0.6 nM

++++

ROCK2, IC50: 1.1 nM

99%+
AT13148 +++

ROCK1, IC50: 6 nM

+++

ROCK2, IC50: 4 nM

PKA 98+%
RKI-1447 +++

ROCK1, IC50: 14.5 nM

+++

ROCK2, IC50: 6.2 nM

99%+
Hydroxyfasudil HCl +

ROCK1, IC50: 0.73 μM

+

ROCK2, IC50: 0.72 μM

PKA 98%
H-1152 2HCl +++

ROCK2, IC50: 0.0120 μM

PKG 99%
GSK269962A HCl ++++

ROCK1, IC50: 1.6 nM

+++

ROCK2, IC50: 4 nM

99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Y-27632 dihydrochloride 生物活性

靶点
  • ROCK1

    ROCK1 (p160ROCK), Ki:140 nM

  • ROCK2

    ROCK2, Ki:300 nM

  • ROCK1

    ROCK1, Ki:140 nM

描述 Y-27632 is a specific inhibitor of Rho-associated kinases[1]. Y-27632 2HCl is the dihydrochloride form of Y-27632 with much higher solubility than Y-27632. It is usually used for ES cell maintance[2], cell reprogramming[3],improving cell suviving after thawing[4], as well as facilitates cell proliferation and migration[5].
作用机制 Y-27632 2HCl can inhibit ROCK1 and ROCK2 in an ATP-competition manner.[1]

Y-27632 dihydrochloride 细胞研究

细胞系 浓度 检测类型 检测时间 活动说明 数据源
C2C12 10 μM Function Assay 6 h Prevents the serine phosphorylation of IRS-1 induced by insulin and/or TNF-α 16267124
CCL39 30 μM Function Assay 30 min Completely abolishes activation of Na-H exchanger NHE1 by integrins 9693382
Cynomolgus monkey embryonic stem cells 20 µM Cytotoxic Assay 24 h Promotes cyES cell survival 18940855
Dbl-d 10 μM Growth Inhibition Assay 18 d Strongly inhibits cell growth 10021386

Y-27632 dihydrochloride 动物研究

Dose Mice: min = 1 mg/kg[8], max = 40 mg/kg[9] Rats: min = 1 mg/kg[10], max = 100 mg/kg[9]
Administration p.o., i.v., i.p.

Y-27632 dihydrochloride 参考文献

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

[2]Li X, Meng G, et al. The ROCK inhibitor Y-27632 enhances the survival rate of human embryonic stem cells following cryopreservation. Stem Cells Dev. 2008 Dec;17(6):1079-85.

[3]Zhao Y, Zhao T, et al. A XEN-like State Bridges Somatic Cells to Pluripotency during Chemical Reprogramming. Cell. 2015 Dec 17;163(7):1678-91.

[4]Gauthaman K, Fong CY, et al. ROCK inhibitor Y-27632 increases thaw-survival rates and preserves stemness and differentiation potential of human Wharton's jelly stem cells after cryopreservation. Stem Cell Rev. 2010 Dec;6(4):665-76.

[5]Wang T, Kang W, et al. Rho-kinase inhibitor Y-27632 facilitates the proliferation, migration and pluripotency of human periodontal ligament stem cells. J Cell Mol Med. 2017 Nov;21(11):3100-3112.

[6]Osei-Owusu P, Knutsen RH, et al. Altered reactivity of resistance vasculature contributes to hypertension in elastin insufficiency. Am J Physiol Heart Circ Physiol. 2014;306(5):H654-66.

[7]Mavria G, Vercoulen Y, et al. ERK-MAPK signaling opposes Rho-kinase to promote endothelial cell survival and sprouting during angiogenesis. Cancer Cell. 2006;9(1):33-44.

Y-27632 dihydrochloride 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.12mL

0.62mL

0.31mL

15.61mL

3.12mL

1.56mL

31.22mL

6.24mL

3.12mL

Y-27632 dihydrochloride 技术信息

CAS号129830-38-2
分子式C14H23Cl2N3O
分子量 320.258
别名 Y-27632 (hydrochloride);Y-27632 2HCl
运输蓝冰
存储条件

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 35 mg/mL(109.29 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

H2O: 100 mg/mL(312.25 mM),配合低频超声助溶

动物实验配方

PO 0.5% CMC-Na 40 mg/mL clear

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