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Y-39983盐酸 /Y-33075 2HCl 99%+

货号:A204681 同义名: Y-39983 Dihydrochloride;Y-33075 Dihydrochloride Ambeed 开学季,买赠积分,赢豪礼

Y-33075 2HCl具有选择性作为 ROCK 抑制剂,IC50 为 3.6 nM。

Y-33075 2HCl 化学结构 CAS号:173897-44-4
Y-33075 2HCl 化学结构
CAS号:173897-44-4
Y-33075 2HCl 3D分子结构
CAS号:173897-44-4
Y-33075 2HCl 化学结构 CAS号:173897-44-4
Y-33075 2HCl 3D分子结构 CAS号:173897-44-4
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Y-33075 2HCl 纯度/质量文件 产品仅供科研

货号:A204681 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-33075 2HCl 生物活性

靶点
  • ROCK

    ROCK, IC50:3.6 nM

描述 Rho-associated kinases (ROCK1 and ROCK2) are serine/threonine kinases that are downstream targets of the small GTPases RhoA, RhoBm and RhoC. ROCKs are involved in diverse cellular activities and irregular ROCK activities could lead to cardiovascular diseases[3]. Y-33075 is a potent and selective ROCK family inhibitor, with an IC50 of 3.6 nM. Y-33075 also inhibits PKC and CaMKII, with IC50 0.42μM and 0.81 μM, respectively[4]. Y-33075 (1 μM) inhibits the contraction of rabbit ciliary artery segments evoked by histamine in Ca2+-free solutions[5]. It also inhibits demyelination and reduces the incidence of relapse episodes in a mouse model of chronic relapsing experimental autoimmune encephalomyelitis (EAE)[6].

Y-33075 2HCl 参考文献

[1]Feng Y, LoGrasso PV, et al. Rho Kinase (ROCK) Inhibitors and Their Therapeutic Potential. J Med Chem. 2016 Mar 24;59(6):2269-300.

[2]Gao C, Huang L, et al. Y-39983, a selective Rho-kinase inhibitor, attenuates experimental autoimmune encephalomyelitis via inhibition of demyelination. Neuroimmunomodulation. 2013;20(6):334-40.

[3]Hartmann, S. et al. The function of Rho-Associated Kinases ROCK1 and Rock2 in the Pathogenesis of Cardiovascular Diseases. Frontiers. 2015.

[4]Hideki Tokushige, et al. Effects of Topical Administration of Y-39983, a Selective Rho-Associated Protein Kinase Inhibitor, on Ocular Tissues in Rabbits and Monkeys Invest. Ophthalmol. Vis. Sci. July 2007 48(7), 3216-3222.

[5]Watabe H, et al. Effects of Rho-associated protein kinase inhibitors Y-27632 and Y-39983 on isolated rabbit ciliary arteries.Jpn J Ophthalmol. Epub. 2011. 55(4), 411-7.

[6]Gao, C., Huang, L., Long, Y., et al. Y-39983, a selective Rho-kinase inhibitor, attenuates experimental autoimmune encephalomyelitis via inhibition of demyelination. Neuroimmunomodulation. 2013. 20(6), 334-340.

Y-33075 2HCl 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.83mL

0.57mL

0.28mL

14.15mL

2.83mL

1.42mL

28.31mL

5.66mL

2.83mL

Y-33075 2HCl 技术信息

CAS号173897-44-4
分子式C16H18Cl2N4O
分子量 353.246
别名 Y-39983 Dihydrochloride;Y-33075 Dihydrochloride
运输蓝冰
存储条件

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 105 mg/mL(297.24 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: 50 mg/mL(141.54 mM),配合低频超声助溶

动物实验配方
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