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/ Hydroxyfasudil/羟基法舒地尔

Hydroxyfasudil/羟基法舒地尔 {[allProObj[0].p_purity_real_show]}

货号：A244270 同义名： HA-1100

Hydroxyfasudil是 Fasudil 的代谢物，是一种强效的 Rho-激酶抑制剂和血管舒张剂。

Hydroxyfasudil/羟基法舒地尔 化学结构 CAS号：105628-72-6
Hydroxyfasudil/羟基法舒地尔 化学结构
CAS号：105628-72-6
Hydroxyfasudil/羟基法舒地尔 3D分子结构
CAS号：105628-72-6
Hydroxyfasudil/羟基法舒地尔 化学结构 CAS号：105628-72-6
Hydroxyfasudil/羟基法舒地尔 3D分子结构 CAS号：105628-72-6
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Hydroxyfasudil/羟基法舒地尔 纯度/质量文件 产品仅供科研

货号：A244270 标准纯度： {[allProObj[0].p_purity_real_show]}
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 HCl ++++

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 2HCl ++

ROCK1, Ki: 140 nM

 		+

ROCK2, Ki: 300 nM

 		99%+
Fasudil HCl +

ROCK2, Ki: 330 nM

 		PKG,Rho 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 95%
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 99%
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。

Hydroxyfasudil/羟基法舒地尔 生物活性

描述 Hydroxyfasudil, a ROCK inhibitor, shows IC50 values of 0.73 and 0.72 μM for ROCK1 and ROCK2, respectively. It less potently inhibits PKA with an IC50 of 37 μM. Hydroxyfasudil enhances eNOS mRNA levels (EC50 of 0.8 ± 0.3 μM), and between 0-100 μM, it increases eNOS activity and stimulates NO production in human aortic endothelial cells (HAEC). At 10 μM, it prolongs the half-life of eNOS mRNA from 13 to 16 hours without affecting eNOS promoter activity [1].
体内研究

Hydroxyfasudil (10 mg/kg, i.p.) significantly increases both average and maximal voided volumes and reduces maximal detrusor pressure in SD rats [2].

Hydroxyfasudil (3 mg/kg, i.p) inhibits hypercontractility induced by norepinephrine in spontaneously hypertensive rats (SHRs), and at doses of 3 and 10 mg/kg, it significantly improves decreased penile cGMP levels in these rats [3].
体外研究

Hydroxyfasudil, a ROCK inhibitor, shows IC50 values of 0.73 and 0.72 μM for ROCK1 and ROCK2, respectively. It less potently inhibits PKA with an IC50 of 37 μM. Hydroxyfasudil enhances eNOS mRNA levels (EC50 of 0.8 ± 0.3 μM), and between 0-100 μM, it increases eNOS activity and stimulates NO production in human aortic endothelial cells (HAEC). At 10 μM, it prolongs the half-life of eNOS mRNA from 13 to 16 hours without affecting eNOS promoter activity [1].

Hydroxyfasudil/羟基法舒地尔 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.

[2]Masago T, et al. Effect of the rho-kinase inhibitor hydroxyfasudil on bladder overactivity: an experimental rat model. Int J Urol. 2009 Oct;16(10):842-7.

[3]Saito M, et al. Hydroxyfasudil ameliorates penile dysfunction in the male spontaneously hypertensive rat. Pharmacol Res. 2012 Oct;66(4):325-31.

Hydroxyfasudil/羟基法舒地尔 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.25mL

0.65mL

0.33mL

16.27mL

3.25mL

1.63mL

32.53mL

6.51mL

3.25mL

Hydroxyfasudil/羟基法舒地尔 技术信息

CAS号105628-72-6
分子式C14H17N3O3S
分子量 307.37
SMILES Code O=C1NC=CC2=C1C=CC=C2S(=O)(N3CCNCCC3)=O
MDL No. MFCD01752417
别名 HA-1100
运输蓝冰
InChI Key ZAVGJDAFCZAWSZ-UHFFFAOYSA-N
Pubchem ID 3064778
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Sealed in dry,2-8°C
溶解方案

DMSO: 30 mg/mL(97.6 mM)，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

Tags: Hydroxyfasudil | 105628-72-6 | HA-1100 | HA1100 | HA 1100 | ROCK Inhibitor | Cell Cycle/DNA Damage | TGF-beta/Smad | Stem Cell/Wnt | Cytoskeleton | ROCK | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Hydroxyfasudil/羟基法舒地尔 纯度/质量文件 | Hydroxyfasudil/羟基法舒地尔 亚型比较 | Hydroxyfasudil/羟基法舒地尔 生物活性 | Hydroxyfasudil/羟基法舒地尔 参考文献 | Hydroxyfasudil/羟基法舒地尔 实验方案 | Hydroxyfasudil/羟基法舒地尔 技术信息

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