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Hydroxyfasudil HCl

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Chemical Structure| 155558-32-0 同义名 : RHO-激酶抑制剂 ;HA-1100 hydrochloride;HA-1100 (hydrochloride);HA1100;Hydroxyfasudil HCl, HA-1100 HCl;Hydroxyfasudil hydrochloride
CAS号 : 155558-32-0
货号 : A591593
分子式 : C14H18ClN3O3S
纯度 : 98%
分子量 : 343.829
MDL号 : MFCD06411567
存储条件：

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 30 mg/mL(87.25 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: 3 mg/mL(8.73 mM)，配合低频超声，并水浴加热至45℃助溶
动物实验配方：
生物活性
靶点

  • ROCK1

    ROCK1, IC50:0.73 μM

  • ROCK2

    ROCK2, IC50:0.72 μM
描述 Hydroxyfasudil hydrochloride acts as a ROCK inhibitor with IC50 values of 0.73 μM for ROCK1 and 0.72 μM for ROCK2. It inhibits PKA less potently, with an IC50 of 37 μM, which is 50 times higher than those for ROCKs. Hydroxyfasudil raises eNOS mRNA levels, exhibiting an EC50 of 0.8 ± 0.3 μM. It also enhances eNOS activity and stimulates NO production in human aortic endothelial cells (HAEC) in a concentration-dependent manner across 0-100 μM. At a concentration of 10 μM, Hydroxyfasudil prolongs the half-life of eNOS mRNA from 13 to 16 hours, without influencing eNOS promoter activity within the range of 0.1 to 100 μM [1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.91mL

0.58mL

0.29mL

14.54mL

2.91mL

1.45mL

29.08mL

5.82mL

2.91mL
参考文献

[1]Rikitake Y, et al. Inhibition of Rho kinase (ROCK) leads to increased cerebral blood flow and stroke protection. Stroke. 2005 Oct;36(10):2251-7. Epub 2005 Sep 1.