DC Chemicals · Product datasheet

Hydroxyfasudil (hydrochloride) — Datasheet

CAT. NO. DC9614

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ParameterValue
Chemical NameHydroxyfasudil HCl
CAS No.155558-32-0
Synonyms1(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
FormulaC14H18ClN3O3S
M.Wt343.826
SMILESCl[H].S(C1=C([H])C([H])=C([H])C2C(N([H])C([H])=C([H])C1=2)=O)(N1C([H])([H])C([H])([H])N([H])C([H])([H])C([H])([H])C1([H])[H])(=O)=O
Purity>98%
Storage2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Biological Activity

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

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].

References & source

DC Chemicals original product information

Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.

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