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Chemical Structure| 155558-32-0 Chemical Structure| 155558-32-0

Structure of Hydroxyfasudil HCl
CAS No.: 155558-32-0

Chemical Structure| 155558-32-0

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Hydroxyfasudil HCl, metabolite of fasudil, is a potent Rho-kinase inhibitor and vasodilator.

Synonyms: HA-1100 hydrochloride; HA1100; Hydroxyfasudil hydrochloride

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Product Details of Hydroxyfasudil HCl

CAS No. :155558-32-0
Formula : C14H18ClN3O3S
M.W : 343.83
SMILES Code : O=C1NC=CC2=C1C=CC=C2S(=O)(N3CCNCCC3)=O.[H]Cl
Synonyms :
HA-1100 hydrochloride; HA1100; Hydroxyfasudil hydrochloride
MDL No. :MFCD06411567
InChI Key :XWWFOUVDVJGNNG-UHFFFAOYSA-N
Pubchem ID :11371328

Safety of Hydroxyfasudil HCl

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302
Precautionary Statements:P280-P305+P351+P338

Related Pathways of Hydroxyfasudil HCl

cytoskeleton

Isoform Comparison

Biological Activity

Target
  • ROCK1

    ROCK1, IC50:0.73 μM

  • ROCK2

    ROCK2, IC50:0.72 μM

In Vitro:

Cell Line
Concentration Treated Time Description References
Bovine aortic endothelial cells (BAEC) 0.1 to 100 μmol/L 48 hours Did not affect eNOS promoter activity Stroke. 2005 Oct;36(10):2251-7
Human saphenous vein endothelial cells (HSVEC) 10 μmol/L 18 hours Increased eNOS mRNA expression to 156±20% Stroke. 2005 Oct;36(10):2251-7
Human umbilical vein endothelial cells (HUVEC) 10 μmol/L 18 hours Increased eNOS mRNA expression to 160±10% Stroke. 2005 Oct;36(10):2251-7
Human aortic endothelial cells (HAEC) 0.1 to 100 μmol/L 18 hours Increased eNOS mRNA and protein expression, resulting in a 1.9- and 1.6-fold increase, respectively, at 10 μmol/L Stroke. 2005 Oct;36(10):2251-7
Bovine aortic endothelial cells 10 μmol/L 24 hours Inhibited hyperglycemia-induced PAI-1 promoter activity Circulation. 2005 Jun 21;111(24):3261-8
Human saphenous vein endothelial cells (HSVECs) 10 μmol/L 24 hours Inhibited hyperglycemia-induced PAI-1 mRNA expression Circulation. 2005 Jun 21;111(24):3261-8
Guinea-pig atria 10^-7 – 10^-4 M Evaluate effects on atrial contractility and heart rate, results showed no significant effects Br J Pharmacol. 2001 Dec;134(8):1724-30
bovine aortic endothelial cells (BAECs) 30 μmol/L 60 minutes HF treatment led to a 4-fold increase in NO2 production, which was completely blocked by the PI3-kinase inhibitor LY294002 or the Akt inhibitor SH-5. Arterioscler Thromb Vasc Biol. 2004 Oct;24(10):1842-7
human saphenous endothelial cells 1 to 100 μmol/L 30 minutes HF increased Akt serine-473 phosphorylation in a concentration-dependent manner, with a 3.4-fold increase at 30 μmol/L. Arterioscler Thromb Vasc Biol. 2004 Oct;24(10):1842-7
rat basilar arteries 3 μmol/L 60 minutes partially restored endothelium-dependent ACh-induced relaxations under hypoxia J Cereb Blood Flow Metab. 2007 May;27(5):998-1009
mouse aorta 3 μmol/L 90 minutes (including 60 minutes hypoxia) partially restored endothelium-dependent ACh-induced relaxations under hypoxia J Cereb Blood Flow Metab. 2007 May;27(5):998-1009

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Dogs Anesthetized open-chest dogs with LAD stenosis model Intravenous infusion 0.1 and 0.3 mg/kg Single dose, 30 minutes duration Evaluate effects on myocardial ischemia, results showed Hydroxyfasudil suppressed ST-segment depression and increased regional myocardial blood flow Br J Pharmacol. 2001 Dec;134(8):1724-30
Mice Distal middle cerebral artery occlusion model Intraperitoneal injection 10 mg/kg Single dose, 60 minutes before or immediately after dMCAO Reduced the area of severely ischemic cortex, improved CBF, eNOS-dependent J Cereb Blood Flow Metab. 2007 May;27(5):998-1009

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.91mL

0.58mL

0.29mL

14.54mL

2.91mL

1.45mL

29.08mL

5.82mL

2.91mL

References

 

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