HYDROXYFASUDIL
Hydroxyfasudil
CAS: 105628-72-6
Molecular Formula: C14H17N3O3S
HYDROXYFASUDIL - Names and Identifiers
HYDROXYFASUDIL - Physico-chemical Properties
| 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. |
HYDROXYFASUDIL - Preparation solution concentration reference
| 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 |
Last Update：2024-01-02 23:10:35
HYDROXYFASUDIL - Reference Information
| 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. |
Last Update：2024-04-09 19:05:03
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