Molecular Formula | C14H17N3O3S |
Molar Mass | 307.37 |
Storage Condition | Sealed in dry,Store in freezer, under -20°C |
In vitro study | Hydroxyfasudil is a ROCK inhibitor, with IC 50 s of 0.73 and 0.72 μM for ROCK1 and ROCK2, respectively. Hydroxyfasudil also less potently inhibits PKA, with an IC 50 of 37 μM, 50-fold higher than those of the ROCKs. Hydroxyfasudil increases eNOS mRNA levels, with an EC 50 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. |
In vivo study | 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. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 3.253 ml | 16.267 ml | 32.534 ml |
5 mM | 0.651 ml | 3.253 ml | 6.507 ml |
10 mM | 0.325 ml | 1.627 ml | 3.253 ml |
5 mM | 0.065 ml | 0.325 ml | 0.651 ml |
biological activity | Hydroxyfasudil is a ROCK inhibitor that can inhibit the activity of ROCK1 and ROCK2 with IC50 values of 0.73 and 0.72 μM respectively. |
target | ROCK2 0.72 μ m (IC 50 ) ROCK1 0.73 μ m (IC 50 ) PKA 37 μ m (IC 50 ) |
in vitro study | Hydroxyfasudil is a ROCK inhibitor, with IC 50 s of 0.73 and 0.72 μ m for ROCK1 and ROCK2, respectively. Hydroxyfasudil also less potently inhibits PKA, with an IC 50 of 37 μ m, 50-fold higher than that of the ROCKs. Hydroxyfasudil increases eNOS mRNA levels, with an EC 50 value of 0.8±0.3 μM. Hydroxyfasudil (0-100μM) concentration-dependently increases eNOS activity and stimulates NO production in human aurtic 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 μ m. |
in vivo study | 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. |