105628-72-6
105628-72-6 structure
- Name: Hydroxyfasudil
- Chemical Name: 5-(1,4-diazepan-1-ylsulfonyl)-2H-isoquinolin-1-one
- CAS Number: 105628-72-6
- Molecular Formula: C14H17N3O3S
- Molecular Weight: 307.36800
- Catalog: Signaling Pathways Cell Cycle/DNA Damage ROCK
- Create Date: 2018-12-27 14:18:13
- Modify Date: 2024-01-07 16:28:57
-
Hydroxyfasudil is a ROCK inhibitor, with IC50s of 0.73 and 0.72 μM for ROCK1 and ROCK2, respectively.
| Name | 5-(1,4-diazepan-1-ylsulfonyl)-2H-isoquinolin-1-one |
|---|---|
| Synonyms |
hfs
hydroxyfasudil ha 1100 Fasudil Impurity 7 |
| Description | Hydroxyfasudil is a ROCK inhibitor, with IC50s of 0.73 and 0.72 μM for ROCK1 and ROCK2, respectively. |
|---|---|
| Related Catalog | |
| Target |
ROCK2:0.72 μM (IC50) ROCK1:0.73 μM (IC50) PKA:37 μM (IC50) |
| 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[1]. |
| 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[2]. 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[3]. |
| Animal Admin | Micturition behavior is studied after intraperitoneal injection of either Hydroxyfasudil (10 mg/kg) or a corresponding volume of saline. Each rat is placed in a metabolic cage containing a urine collection funnel that is placed over an electronic balance. The balance is connected to a personal computer via a multiport controller and used to measure the cumulative weight of the collected urine. Every 150 s during a continuous 24-h period, the computer samples and records the data for the micturition frequency and volumes. The micturition reflex parameters that are collected includ: urine volume per micturition, maximal micturition volume, micturition frequency, and total urine output in the Hydroxyfasudil- or vehicle-treated animals. Each monitoring session started at 18.00 hours. Prior to being placed in the metabolic cage at the start of each experimental period, the animals receive either a single injection of Hydroxyfasudil (10 mg/kg) dissolved in saline or an injection of saline without the inhibitor[2]. |
| References |
| Density | 1.329g/cm3 |
|---|---|
| Boiling Point | 613.7ºC at 760mmHg |
| Molecular Formula | C14H17N3O3S |
| Molecular Weight | 307.36800 |
| Flash Point | 325ºC |
| Exact Mass | 307.09900 |
| PSA | 90.65000 |
| LogP | 1.85960 |
| Vapour Pressure | 9.04E-16mmHg at 25°C |
| Storage condition | 2-8°C |
| HS Code | 2933990090 |
|---|
| HS Code | 2933990090 |
|---|---|
| Summary | 2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0% |