Hydroxyfasudil HCl

Catalog No.S8208 Batch:S820801

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Technical Data

Formula

C14H17N3O3S·HCl·xH2O
Molecular Weight 343.83 CAS No. 155558-32-0
Solubility (25°C)* In vitro DMSO 68 mg/mL (197.77 mM)
Water 60 mg/mL (174.5 mM)
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description Hydroxyfasudil HCl, an active metabolite of fasudil hydrochloride, is a specific Rho-kinase(ROCK) inhibitor with IC50 values of 0.73 μM and 0.72 μM for ROCK1 and ROCK2, respectively.
Targets
ROCK2 [1]
(Cell-free assay)		 ROCK1 [1]
(Cell-free assay)		 PKA [1]
(Cell-free assay)
0.72 μM 0.73 μM 37 μM
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)[1]. 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)[3].
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[2]. HF protects the myocardium subjected to pacing-induced ischaemia through the increase in the regional myocardial blood flow[3].

Protocol (from reference)

Cell Assay:[1]
  • Cell lines

    Human vascular endothelial cells

  • Concentrations

    0.1 to 100 μmol/L

  • Incubation Time

    18 h

  • 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.

Animal Study:[2]
  • Animal Models

    Mongrel dogs

  • Dosages

    10, 30, and 100 μg/kg

  • Administration

    IC（Intracoronary administration）

Selleck's Hydroxyfasudil HCl has been cited by 2 publications

Pixantrone as a novel MCM2 inhibitor for ovarian cancer treatment [ Eur J Pharmacol, 2024, 979:176835] PubMed: 39032764
Drug and siRNA screens identify ROCK2 as a therapeutic target for ciliopathies [ bioRxiv, 2020, 10.1101/2020.11.26.393801] PubMed: N/A

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.