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Hydroxyfasudil

In stock
Catalog No.
A3478
Rho-kinase inhibitor and vasodilator
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$160.00
In stock
5mg
$146.00
In stock
10mg
$177.00
In stock
50mg
$772.00
In stock

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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

StorageStore at -20°C
M.Wt307.37
Cas No.105628-72-6
FormulaC14H17N3O3S
SynonymsHA-1100;HA 1100;HA1100
SolubilitySoluble in DMSO
Chemical Name5-(1,4-diazepan-1-ylsulfonyl)-2H-isoquinolin-1-one
SDFDownload SDF
Canonical SMILESC1CNCCN(C1)S(=O)(=O)C2=CC=CC3=C2C=CNC3=O
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Quality Control

Quality Control & MSDS

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Chemical structure

Hydroxyfasudil