| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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Purity: ≥98%
Hydroxyfasudil (also called HA1100 HCl), a metabolite of Fasudil, is a potent Rho-kinase inhibitor and vasodilator. It inhibits ROCK, with IC50 values for ROCK1 and ROCK2 of 0.73 and 0.72 μM, respectively. When under hypoxia, hydroxyfasudil stops endothelial NO synthase (eNOS) from being downregulated. At 10 μmol/L, hydroxyfasudil causes a concentration-dependent increase in eNOS mRNA and protein expression, measuring 1.9 and 1.6 fold increases, respectively. A 1.5- and 2.3-fold increase in eNOS activity and NO production, respectively, are correlated with this.
| Targets |
ROCK2 (IC50 = 0.72 μM); ROCK1 (IC50 = 0.73 μM); PKA (IC50 = 37 μM)
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| ln Vitro |
Hydroxyfasudil is a ROCK inhibitor, with IC50 values for ROCK1 and ROCK2 of 0.73 and 0.72 μM, respectively. Moreover, hydroxyfasudil inhibits PKA less potently than ROCKs, with an IC50 of 37 μM, which is 50 times higher. The eNOS mRNA levels are increased by hydroxyfasudil, which has an EC50 value of 0.8 ± 0.3 μM. Human aortic endothelial cells (HAEC) produce more NO and exhibit an increase in eNOS activity in response to hydroxyfasudil (0-100 μM) concentration. At concentrations of 0.1 to 100 μM, hydroxyfasudil (10 μM) has no effect on eNOS promoter activity, but it lengthens the half-life of eNOS mRNA from 13 to 16 hours[1].
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| ln Vivo |
Hydroxyfasudil (10 mg/kg, i.p.) amatically raises the average and maximal voided volumes in SD rats. Moreover, the maximal detrusor pressure is significantly reduced by hydroxyfasudil[2]. Among spontaneously hypertensive rats (SHRs), hydroxyfasudil (3 mg/kg, i.p.) suppresses norepinephrine-induced hypercontractility. Furthermore, Hydroxyfasudil (3, 10 mg/kg, i.p) significantly restores rats' lower penile cGMP contents[3].
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| Enzyme Assay |
Hydroxyfasudil HCl (also called HA1100 HCl), a metabolite of Fasudil, is a strong vasodilator and Rho-kinase inhibitor. With IC50s of 0.73 and 0.72 μM for ROCK1 and ROCK2, respectively, it inhibits ROCK. In hypoxic environments, hydroxyfasudil inhibits the downregulation of endothelial NO synthase (eNOS). Hydroxyfasudil stimulates eNOS mRNA and protein expression in a concentration-dependent manner; at 10 μmol/L, this leads to a 1.9- and 1.6-fold increase, respectively. This corresponds to a 1.5- and 2.3-fold rise in NO production and eNOS activity, respectively.
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| Cell Assay |
The expression and activity of eNOS are measured after hydroxyfasudil is added to human vascular endothelial cells at varying concentrations (0.1 to 100 μmol/L).
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| Animal Protocol |
The behavior of micturition is examined following an intraperitoneal injection of saline or Hydroxyfasudil (10 mg/kg). Every rat has its own metabolic cage with a urine collection funnel set above an electronic balance. The cumulative weight of the pee collected is measured by the balance, which is connected to a PC via a multiport controller. The computer takes a sample and stores the data for the micturition frequency and volumes every 150 s over the course of a 24-hour period. The micturition reflex parameters that are measured in animals treated with Hydroxyfasudil or a vehicle include total urine output, frequency of micturitions, maximal micturition volume, and urine volume per micturition. Every monitoring session began at eighteen minutes to the hour. The animals receive either an injection of saline without the inhibitor or a single injection of Hydroxyfasudil (10 mg/kg) dissolved in saline prior to being placed in the metabolic cage at the beginning of each experimental period[2].
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| References |
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| Molecular Formula |
C14H17N3O3S
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| Molecular Weight |
307.37
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| Exact Mass |
307.10
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| Elemental Analysis |
C, 54.71; H, 5.58; N, 13.67; O, 15.62; S, 10.43
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| CAS # |
105628-72-6
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| Related CAS # |
Hydroxyfasudil hydrochloride;155558-32-0
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| Appearance |
Solid powder
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| SMILES |
C1CNCCN(C1)S(=O)(=O)C2=CC=CC3=C2C=CNC3=O
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| InChi Key |
ZAVGJDAFCZAWSZ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C14H17N3O3S/c18-14-12-3-1-4-13(11(12)5-7-16-14)21(19,20)17-9-2-6-15-8-10-17/h1,3-5,7,15H,2,6,8-10H2,(H,16,18)
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| Chemical Name |
5-(1,4-diazepan-1-ylsulfonyl)-2H-isoquinolin-1-one
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.5 mg/mL (1.63 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 5.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 0.5 mg/mL (1.63 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 5.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 0.5 mg/mL (1.63 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.2534 mL | 16.2670 mL | 32.5341 mL | |
| 5 mM | 0.6507 mL | 3.2534 mL | 6.5068 mL | |
| 10 mM | 0.3253 mL | 1.6267 mL | 3.2534 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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