HYDROXYFASUDIL MONOHYDROCHLORIDE
HYDROXYFASUDIL MONOHYDROCHLORIDE
CAS: 155558-32-0
Molecular Formula: C14H18ClN3O3S
HYDROXYFASUDIL MONOHYDROCHLORIDE - Names and Identifiers
HYDROXYFASUDIL MONOHYDROCHLORIDE - Physico-chemical Properties
| Molecular Formula | C14H18ClN3O3S |
| Molar Mass | 343.82902 |
| Melting Point | >250 (dec.) |
| Solubility | H2O: >5mg/mL |
| Appearance | solid |
| Color | white |
| Storage Condition | Inert atmosphere,2-8°C |
| In vitro study | Hydroxyfasudil hydrochloride 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 MONOHYDROCHLORIDE - Risk and Safety
| Hazard Symbols | Xn - Harmful |
| Risk Codes | 22 - Harmful if swallowed |
| WGK Germany | 3 |
HYDROXYFASUDIL MONOHYDROCHLORIDE - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.908 ml | 14.542 ml | 29.084 ml |
| 5 mM | 0.582 ml | 2.908 ml | 5.817 ml |
| 10 mM | 0.291 ml | 1.454 ml | 2.908 ml |
| 5 mM | 0.058 ml | 0.291 ml | 0.582 ml |
Last Update：2024-01-02 23:10:35
HYDROXYFASUDIL MONOHYDROCHLORIDE - Reference Information
| biological activity | Hydroxyfasudil hydrochloride is a ROCK inhibitor that inhibits the activity of ROCK1 and rock2, the IC50 values were 0.73 and 0.72 μm, respectively. |
| Target | ROCK2 0.72 μm (IC 50 ) ROCK1 0.73 μm (IC 50 ) PKA 37 μm (IC 50 ) |
| in vitro study | hydroxy fasudil hydrogel is a ROCK inhibitor, with IC 50 s of 0.73 and 0.72 μm for ROCK1 and ROCK2, review. Hydroxyfasudil also less Pot alone affected PKA, with an IC 50 of 37 μm, 50-fold higher than those of the ROCKs. Hydroxyfasudil creases 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 | hydroxy fasudil (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. Hydroxy fasudil (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：2024-04-10 22:30:50
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