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Hydroxyfasudil

SKU: orb1219150

Description

Hydroxyfasudil is a ROCK inhibitor(IC50s of 0.73 and 0.72 μM for ROCK1 and ROCK2, respectively).

Images & Validation

Key Properties

CAS Number105628-72-6
MW307.37
Purity>98% (HPLC)
FormulaC14H17N3O3S
SMILESO=C1NC=CC2=C1C=CC=C2S(=O)(N3CCNCCC3)=O
TargetPKA
SolubilityDMSO:31 mg/mL (100.86 mM)

Bioactivity

In Vivo
Hydroxyfasudil (10 mg/kg, i.p.) significantly increases both the average and maximal voided volumes in SD rats. Hydroxyfasudil also significantly decreases the maximal detrusor pressure. Hydroxyfasudil (3 mg/kg, i. p) inhibits hypercontractility induced by norepinephrine in spontaneously hypertensive rats (SHRs). Furthermore, Hydroxyfasudil (3, 10 mg/kg, i. p) significantly ameliorates decreased penile cGMP contents in rats.
In Vitro
Hydroxyfasudil is a ROCK inhibitor, with IC50s of 0.73 and 0.72 μM for ROCK1 and ROCK2, respectively. Hydroxyfasudil also less potently inhibits PKA, with an IC50 of 37 μM, 50-fold higher than those of the ROCKs. Hydroxyfasudil increases eNOS mRNA levels, with an EC50 value of 0.8 ± 0.3 μM. Hydroxyfasudil (0-100 μM) concentration-dependently increases eNOS activity and stimulates NO production in human aortic endothelial cells (HAEC). Hydroxyfasudil (10 μM) increases the half-life of eNOS mRNA from 13 to 16 hours, but does not affect eNOS promoter activity at concentrations from 0.1 to 100 μM.

Storage & Handling

StorageStorage temperature: -20°C. Stability: ≥ 2 years
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

HA-1100 | Hydroxy-Fasudil

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Hydroxyfasudil (orb1219150)

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