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Y-33075 2HCl

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Chemical Structure| 173897-44-4 同义名 : Y-39983 Dihydrochloride;Y-33075 Dihydrochloride
CAS号 : 173897-44-4
货号 : A204681
分子式 : C16H18Cl2N4O
纯度 : 99%+
分子量 : 353.246
MDL号 : MFCD00945328
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：
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].
实验方案
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
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.