Hydroxyfasudil 羟基法舒地尔; HA-1100|cas:105628-72-6|西域试剂

Hydroxyfasudil 羟基法舒地尔; HA-1100,98.42%

产品编号：Bellancom-13911| CAS NO：105628-72-6| 分子式：C₁₄H₁₇N₃O₃S| 分子量：307.37

Hydroxyfasudil 是一种 ROCK 抑制剂，可抑制 ROCK1 和 ROCK2 的活性，IC50 值分别为 0.73 和 0.72 μM。

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货号	价格	库存与货期
Bellancom-13911	￥865.00	杭州北京（现货）
Bellancom-13911	￥1051.00	杭州北京（现货）
Bellancom-13911	￥4604.00	杭州北京（现货）

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Hydroxyfasudil 羟基法舒地尔; HA-1100

产品介绍

Hydroxyfasudil 是一种 ROCK 抑制剂，可抑制 ROCK1 和 ROCK2 的活性，IC₅₀ 值分别为 0.73 和 0.72 μM。

生物活性

Hydroxyfasudil is a ROCK inhibitor, with IC₅₀s of 0.73 and 0.72 μM for ROCK1 and ROCK2, respectively.

体外研究

Hydroxyfasudil is a ROCK inhibitor, with IC₅₀s of 0.73 and 0.72 μM for ROCK1 and ROCK2, respectively. Hydroxyfasudil also less potently inhibits PKA, with an IC₅₀ of 37 μM, 50-fold higher than those of the ROCKs. Hydroxyfasudil increases eNOS mRNA levels, with an EC₅₀ value of 0.8 ± 0.3 μM. Hydroxyfasudil (0-100 μM) concentration-dependently increases eNOS activity and stimulates NO production in human aortic endothelial cells (HAEC). Hydroxyfasudil (10 μM) increases the half-life of eNOS mRNA from 13 to 16 hours, but does not affect eNOS promoter activity at concentrations from 0.1 to 100 μM.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

Hydroxyfasudil (10 mg/kg, i.p.) significantly increases both the average and maximal voided volumes in SD rats. Hydroxyfasudil also significantly decreases the maximal detrusor pressure. Hydroxyfasudil (3 mg/kg, i.p) inhibits hypercontractility induced by norepinephrine in spontaneously hypertensive rats (SHRs). Furthermore, Hydroxyfasudil (3, 10 mg/kg, i.p) significantly ameliorates decreased penile cGMP contents in rats.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

性状

Solid

溶解性数据

In Vitro:

DMSO : ≥ 31 mg/mL (100.86 mM)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.2534 mL	16.2670 mL	32.5341 mL
5 mM	0.6507 mL	3.2534 mL	6.5068 mL
10 mM	0.3253 mL	1.6267 mL	3.2534 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 0.5 mg/mL (1.63 mM); Clear solution

此方案可获得 ≥ 0.5 mg/mL (1.63 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 5.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 0.5 mg/mL (1.63 mM); Clear solution

此方案可获得 ≥ 0.5 mg/mL (1.63 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 5.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 0.5 mg/mL (1.63 mM); Clear solution

此方案可获得 ≥ 0.5 mg/mL (1.63 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 5.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在西域网站选购。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

参考文献

. 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. [Content Brief]

. 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. [Content Brief]

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

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Hydroxyfasudil 羟基法舒地尔; HA-1100,98.42%

Hydroxyfasudil 羟基法舒地尔; HA-1100

化学品安全说明书(MSDS)

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