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Hydroxyfasudil hydrochloride

Catalog No.
A3479
Rho-kinase inhibitor and vasodilator
Grouped product items
Size Price Stock Qty
10mg
Special Price $47.25 Regular Price $105.00
In stock
50mg
Special Price $207.00 Regular Price $460.00
In stock
For scientific research use only and should not be used for diagnostic or medical purposes.

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Background

Description: IC50 Value: 0.12 uM (ROCK1); 0.17 uM (ROCK2) [1] Hydroxyfasudil, metabolite of Fasudil, is a potent Rho-kinase inhibitor and vasodilator. in vitro: Fasudil (1-10 μM) and hydroxyfasudil (0.3-10 μM) significantly prevented endothelin-induced cardiomyocyte hypertrophy [2]. Hydroxyfasudil significantly attenuated serotonin (IC)-induced vasoconstriction of SA (-7 +/- 1% vs. 2 +/- 1%, p < 0.01). Coronary I/R significantly impaired coronary vasodilation to acetylcholine after I/R (SA, p < 0.05; and A, p < 0.01 vs. before I/R) and L-NMMA further reduced the vasodilation, whereas hydroxyfasudil completely preserved the responses. in vivo: Treatment with hydroxyfasudil significantly improved bladder intercontraction intervals. Rats treated with hydroxyfasudil also showed a significant reduction of histopathological features associated with cystitis [3]. Twelve-week-old male SHRs were treated with hydroxyfasudil (3 or 10 mg/kg, i.p.) once a day for 6 weeks. Treatment with hydroxyfasudil significantly improved the decreased penile cGMP concentrations, the increased Rho kinase activities, the increased norepinephrine-induced contractions, and the decreased acetylcholine-induced relaxation in a dose-dependent manner [4]. Toxicity: The proportion of patients with good clinical outcome was 74.5% (41/55) in the fasudil group and 61.7% (37/60) in the nimodipine group. There were no serious adverse events reported in the fasudil group [5]. Clinical trial: N/A

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt343.83
Cas No.155558-32-0
FormulaC14H18ClN3O3S
SynonymsHA-1100 hydrochloride;HA 1100 hydrochloride;HA1100 hydrochloride
Solubilityinsoluble in EtOH; ≥7.88 mg/mL in DMSO with gentle warming; ≥5.04 mg/mL in H2O with gentle warming and ultrasonic
Chemical Name5-(1,4-diazepan-1-ylsulfonyl)-2H-isoquinolin-1-one;hydrochloride
SDFDownload SDF
Canonical SMILESC1CNCCN(C1)S(=O)(=O)C2=CC=CC3=C2C=CNC3=O.Cl
Shipping ConditionSmall Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips We do not recommend long-term storage for the solution, please use it up soon.

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