Hydroxy Fasudil Hydrochloride

Modify Date: 2024-01-04 18:27:26

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

 Use of Hydroxy Fasudil Hydrochloride


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

 Names

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

 Hydroxy Fasudil Hydrochloride Biological Activity

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

 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)