Hydroxy Fasudil Hydrochloride

Names

[ Name ]:
Hydroxy Fasudil Hydrochloride

[Synonym ]:
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)

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]:

Signaling Pathways >> Cell Cycle/DNA Damage >> ROCK

Signaling Pathways >> Stem Cell/Wnt >> ROCK

Signaling Pathways >> TGF-beta/Smad >> ROCK

Research Areas >> Cardiovascular Disease

Research 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.

[Related Small Molecules]

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

Related Compounds

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