Hydroxyfasudil (HA-1100) HCl

Catalog No.S8208

Hydroxyfasudil (HA-1100) HCl Chemical Structure

Molecular Weight(MW): 343.83

Hydroxyfasudil (HA-1100), 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.

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Biological Activity

Description Hydroxyfasudil (HA-1100), 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

Cell Research:[1]
+ Expand
  • 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.
    (Only for Reference)
Animal Research:[2]
+ Expand
  • Animal Models: Mongrel dogs
  • Formulation: Physiologic saline
  • Dosages: 10, 30, and 100 μg/kg
  • Administration: IC(Intracoronary administration)
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 68 mg/mL warmed (197.77 mM)
Water 60 mg/mL warmed (174.5 mM)
Ethanol 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.

Chemical Information

Molecular Weight 343.83
Formula

C14H17N3O3S·HCl·xH2O

CAS No. 155558-32-0 (HCl salt)
Storage powder
Synonyms N/A

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ROCK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID