| Name | Hydroxyfasudil Hydrochloride |
| Description | Hydroxyfasudil Hydrochloride (HA 1100 hydrochloride) is a ROCK1/2 inhibitor (IC50s: 0.73/0.72 μM). |
| Animal Research | Hydroxyfasudil is formulated in saline.Micturition behavior is studied after administration of either Hydroxyfasudil (10 mg/kg, i.p.) 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 include: 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 received either a single injection of Hydroxyfasudil (10 mg/kg) dissolved in saline or an injection of saline without the inhibitor. |
| In vitro | Hydroxyfasudil has a weak inhibition of PKA (IC50: 37 μM), 50-fold higher than those of the ROCKs. Hydroxyfasudil increases eNOS mRNA levels (EC50: 0.8 ± 0.3 μM). Hydroxyfasudil (0-100 μM) concentration-dependently increases eNOS activity and stimulates NO production in HAEC. Hydroxyfasudil (10 μM) increases the half-life of eNOS mRNA from 13 to 16 hours but does not affect eNOS promoter activity (0.1-100 μM). |
| In vivo | Hydroxyfasudil (10 mg/kg, i.p.) markedly increases both the maximal and average voided volumes and reduces maximal detrusor pressure in SD rats. In spontaneously hypertensive rats (SHRs), Hydroxyfasudil (3 mg/kg, i.p.) inhibits norepinephrine-induced hypercontractility and significantly ameliorates decreased penile cGMP contents at doses of 3/10 mg/kg, i.p. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 62 mg/mL (180.32 mM), Sonication is recommended.
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| Keywords | ROK | ROCK | Rho-kinase | Rho-associated protein kinase | Rho-associated kinase | Inhibitor | inhibit | Hydroxyfasudil Hydrochloride | Hydroxyfasudil | HA-1100 Hydrochloride | HA1100 Hydrochloride | HA-1100 | HA1100 | HA 1100 Hydrochloride | HA 1100 |
| Inhibitors Related | SB-747651A Dihydrochloride | GSK180736A | Fasudil | SAR407899 hydrochloride | RKI-1447 | Belumosudil | Fasudil hydrochloride | Y-27632 dihydrochloride | Tofacitinib | Y-27632 | ROCK-IN-5 | Thiazovivin |
| Related Compound Libraries | Target-Focused Phenotypic Screening Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Kinase Inhibitor Library | Inhibitor Library | NO PAINS Compound Library | Bioactive Compounds Library Max | Cell Cycle Compound Library | Cytoskeletal Signaling Pathway Compound Library | Anti-Cancer Compound Library | Anti-Metabolism Disease Compound Library | TGF-beta/Smad Compound Library |
United States
