Hydroxyfasudil Hydrochloride

SKU: orb1223271

Description

Hydroxyfasudil hydrochloride is a ROCK1/2 inhibitor (IC50s: 0.73/0.72 μM).

Images & Validation

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Key Properties

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CAS Number	155558-32-0
MW	343.83
Purity	>98% (HPLC)
Formula	C₁₄H₁₈ClN₃O₃S
SMILES	C1CNCCN(C1)S(=O)(=O)C2=CC=CC3=C2C=CNC3=O.Cl
Target	PPAR
Solubility	DMSO : 30 mg/mL. 87.25 mM;

Bioactivity

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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 hydrochloride 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

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Storage	Storage temperature: -20°C. Stability: ≥ 2 years
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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HA-1100 hydrochloride | HA 1100 hydrochloride

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Gene Symbol

PPAR

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