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Hydroxyfasudil hydrochloride

Cat. No. M5260
Hydroxyfasudil hydrochloride Structure

HA-1100 HCl

Size Price Availability Quantity
5mg USD 89  USD89 In stock
10mg USD 122  USD122 In stock
50mg USD 510  USD510 In stock
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Quality Control
Biological Activity

In vitro: Hydroxyfasudil prevents the downregulation of endothelial NO synthase (eNOS) under hypoxic conditions. In a concentration-dependent manner, hydroxyfasudil increases eNOS mRNA and protein expression, resulting in a 1.9- and 1.6-fold increase, respectively, at 10 μmol/L (P<0.05 for both). This correlates with a 1.5- and 2.3-fold increase in eNOS activity and NO production, respectively (P<0.05 for both). Hydroxyfasudil also inhibits various chemoattractant-induced migration of neutrophils. Hydroxyfasudil potently inhibits Rho-kinase (IC50, 0.9 ± 1.8 μM), while its inhibitory eff€ect is markedly (at least 50 ± 100 times) less for myosin light chain kinase (MLCK) or protein kinase C (PKC).

In vivo: Intracoronary administration of hydroxyfasudil(HF) causes a significant coronary vasodilation of both small arteries and arterioles in a dose-dependent manner under control conditions with a resultant increase in CBF(coronary blood flow). Intracoronary hydroxyfasudil does not significantly alter mean aortic pressure or heart rate. Pretreatment with hydroxyfasudil markedly reduces the I/R-induced myocardial infarct size, and this beneficial effect of hydroxyfasudil is significantly attenuated by L-NMMA. NO may be involved in those cardiovascular protective effects of hydroxyfasudil. Hydroxyfasudil may also be effective for the treatment of pulmonary hypertension. HF protects the myocardium subjected to pacing-induced ischaemia through the increase in the regional myocardial blood flow.

Cell Experiment
Cell lines Human vascular endothelial cells
Preparation method Human vascular endothelial cells are treated with increasing concentrations of hydroxyfasudil (0.1 to 100 μmol/L) and eNOS expression and activity are measured.
Concentrations 0.1 to 100 μmol/L
Incubation time 18 h
Animal Experiment
Animal models Mongrel dogs
Formulation Physiologic saline
Dosages 10, 30, and 100 μg/kg
Administration IC(Intracoronary administration)
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 343.83
Formula C14H17N3O3S·HCl
CAS Number 155558-32-0
Purity 99.82%
Solubility DMSO: ≥ 30 mg/mL
Storage at -20°C

[1] Holmström F, et al. Prostate. Protective effect of hydroxyfasudil, a Rho kinase inhibitor, on ventral prostatic hyperplasia in the spontaneously hypertensive rat.

[2] Shimizu N, et al. Int J Urol. Effects of the Rho kinase inhibitor, hydroxyfasudil, on bladder dysfunction and inflammation in rats with HCl-induced cystitis.

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Keywords: Hydroxyfasudil hydrochloride, HA-1100 HCl supplier, ROCK, inhibitors

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