CAS 155558-32-0|Hydroxy Fasudil Hydrochloride

Introduction：Basic information about CAS 155558-32-0|Hydroxy Fasudil Hydrochloride, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.

Table of Contents

1. Names
2. Hydroxy Fasudil Hydrochloride BiologicalActivity
3. Chemical & Physical Properties
4. Safety Information
5. Synonyms

Common Name	Hydroxy Fasudil Hydrochloride
CAS Number	155558-32-0	Molecular Weight	343.829
Density	/	Boiling Point	/
Molecular Formula	C₁₄H₁₈ClN₃O₃S	Melting Point	>250ºC(dec.)
MSDS	/	Flash Point	/

Names

Name	5-(1,4-diazepan-1-ylsulfonyl)-2H-isoquinolin-1-one,hydrochloride
Synonym	More Synonyms

Hydroxy Fasudil Hydrochloride BiologicalActivity

Description	Hydroxyfasudil hydrochloride is a ROCK inhibitor, with IC50s of 0.73 and 0.72 μM for ROCK1 and ROCK2, respectively.
Related Catalog	Signaling Pathways >>Cell Cycle/DNA Damage >>ROCKSignaling Pathways >>Stem Cell/Wnt >>ROCKSignaling Pathways >>TGF-beta/Smad >>ROCKResearch Areas >>Cardiovascular DiseaseResearch Areas >>Inflammation/Immunology
Target	ROCK2:0.72 μM (IC50) ROCK1:0.73 μM (IC50) PKA:37 μM (IC50)
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[1].
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[2]. 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[3].
Animal Admin	Micturition behavior is studied after intraperitoneal injection of either Hydroxyfasudil (10 mg/kg) or a corresponding volume of saline. Each rat is placed in a metabolic cage containing a urine collection funnel that is placed over an electronic balance. The balance is connected to a personal computer via a multiport controller and used to measure the cumulative weight of the collected urine. Every 150 s during a continuous 24-h period, the computer samples and records the data for the micturition frequency and volumes. The micturition reflex parameters that are collected includ: urine volume per micturition, maximal micturition volume, micturition frequency, and total urine output in the Hydroxyfasudil- or vehicle-treated animals. Each monitoring session started at 18.00 hours. Prior to being placed in the metabolic cage at the start of each experimental period, the animals receive either a single injection of Hydroxyfasudil (10 mg/kg) dissolved in saline or an injection of saline without the inhibitor[2].
References	[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.

Chemical & Physical Properties

Melting Point	>250ºC(dec.)
Molecular Formula	C₁₄H₁₈ClN₃O₃S
Molecular Weight	343.829
Exact Mass	343.075745
PSA	90.91000
LogP	3.07390
InChIKey	XWWFOUVDVJGNNG-UHFFFAOYSA-N
SMILES	Cl.O=c1[nH]ccc2c(S(=O)(=O)N3CCCNCC3)cccc12

Safety Information

Hazard Codes	Xn: Harmful;
Risk Phrases	R22

Synonyms

5-(1,4-Diazepan-1-ylsulfonyl)isoquinolin-1-ol hydrochloride (1:1)

1-(1-Hydroxy-5-isoquinolinesulfonyl)homopiperazine hydrochloride hydrate

5-(1,4-Diazepan-1-ylsulfonyl)-1(2H)-isoquinolinone hydrochloride (1:1)

HA1100 Hydrochloride

HYDROXYFASUDIL

1(2H)-Isoquinolinone, 5-[(hexahydro-1H-1,4-diazepin-1-yl)sulfonyl]-, hydrochloride (1:1)

Hydroxyfasudil monohydrochloride

HA1100

Hydroxy Fasudil Hydrochloride

Fasudil Impurity 7 HCl

Hydroxyfasudil (hydrochloride)

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