Hydroxyfasudil hydrochloride|155558-32-0|(羟基法舒地尔盐酸盐; HA-1100 hydrochloride; HA 1100 hydrochloride; HA1100 hydrochloride)-陌孚医药/Medlife

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Hydroxyfasudil hydrochloride (Synonyms: 羟基法舒地尔盐酸盐; HA-1100 hydrochloride; HA 1100 hydrochloride; HA1100 hydrochloride)

目录号: PC15930 纯度: ≥98%

CAS No. :155558-32-0

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中文名称	Hydroxyfasudil hydrochloride
中文别名	RHO-激酶抑制剂;猪胆酸;羟基法舒地尔盐酸盐;羟基法舒地尔
英文名称	Hydroxyfasudil hydrochloride
英文别名	1(2H)-Isoquinolinone,5-[(hexahydro-1H-1,4-diazepin-1-yl)sulfonyl]-, hydrochloride (1:1);HYDROXYFASUDIL MONOHYDROCHLORIDE;HA 1100 hydrochloride;HA-1100 (hydrochloride);1-(1-Hydroxy-5-isoquinolinesulfonyl)homopiperazine hydrochloride hydrate;HA1100;HA-1100 hydrochloride;HYDROXYFASUDIL;Hydroxyfasudil (HA-1100);Hydroxyfasudil (HA-1100) HCl;Hydroxyfasudil Hydrochloride;Hydroxyfasudil hydrochloride hydrate;5-[(Hexahydro-1H-1,4-diazepin-1-yl)sulfonyl]-1(2H)-isoquinolinone;1-(1-hydroxy-5-isoquinolinesulfonyl)homopiperazine monohydrochloride;Hydroxyfasudil hydrochloride hydrate,1-(1-Hydroxy-5-isoquinolinesulfonyl)homopiperazine hydrochloride hydrate;Hydroxyfasudil (hydrochloride);HA1100 Hydrochloride;Hydroxyfasudil HCl;Hydroxy Fasudil Hydrochloride;1-(1-Hydroxy-5-isoquinolinesulfonyl)homopiperazine, HCl;Hydroxyfasudil(hydrochloride);C14H17N3O3S.ClH;BCP11069;IN1295;3725AH;F
Cas No.	155558-32-0
分子式	C₁₄H₁₈ClN₃O₃S
分子量	343.83
包装储存	4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

生物活性

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

性状

Solid

IC50 & Target[1][2]

ROCK2

0.72 μM (IC₅₀)

ROCK1

0.73 μM (IC₅₀)

PKA

37 μM (IC₅₀)

体外研究(In Vitro)

Hydroxyfasudil hydrochloride 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.

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

体内研究(In Vivo)

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.

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

运输条件

Room temperature or refrigerated transportation.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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. [Information]

[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. [Information]

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

溶解度数据

体外研究:

DMSO : 30 mg/mL (87.25 mM; Need ultrasonic)

H₂O : 3.33 mg/mL (9.69 mM; ultrasonic and warming and heat to 60°C)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.9084 mL	14.5421 mL	29.0841 mL
5 mM	0.5817 mL	2.9084 mL	5.8168 mL
10 mM	0.2908 mL	1.4542 mL	2.9084 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，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 (sealed storage, away from moisture)。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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