Hydroxyfasudil (HA-1100) HCl

Hydroxyfasudil (HA-1100), an active metabolite of fasudil hydrochloride, is a specific Rho-kinase(ROCK) inhibitor with IC50 values of 0.73 μM and 0.72 μM for ROCK1 and ROCK2, respectively.

Hydroxyfasudil (HA-1100) HCl Chemical Structure

Hydroxyfasudil (HA-1100) HCl Chemical Structure

CAS: 155558-32-0

Selleck's Hydroxyfasudil (HA-1100) HCl has been cited by 1 publication

Purity & Quality Control

Batch: S820801 DMSO] 68 mg/mL] false] Water] 60 mg/mL] false] Ethanol] Insoluble] false Purity: 99.09%
99.09

Hydroxyfasudil (HA-1100) HCl Related Products

Signaling Pathway

Choose Selective ROCK Inhibitors

Biological Activity

Description Hydroxyfasudil (HA-1100), an active metabolite of fasudil hydrochloride, is a specific Rho-kinase(ROCK) inhibitor with IC50 values of 0.73 μM and 0.72 μM for ROCK1 and ROCK2, respectively.
Targets
ROCK2 [1]
(Cell-free assay)
ROCK1 [1]
(Cell-free assay)
PKA [1]
(Cell-free assay)
0.72 μM 0.73 μM 37 μM
In vitro
In vitro Hydroxyfasudil prevents the downregulation of endothelial NO synthase (eNOS) under hypoxic conditions. In a concentration-dependent manner, hydroxyfasudil increases eNOS mRNA and protein expression, resulting in a 1.9- and 1.6-fold increase, respectively, at 10 μmol/L (P<0.05 for both). This correlates with a 1.5- and 2.3-fold increase in eNOS activity and NO production, respectively (P<0.05 for both)[1]. Hydroxyfasudil also inhibits various chemoattractant-induced migration of neutrophils. Hydroxyfasudil potently inhibits Rho-kinase (IC50, 0.9 ± 1.8 μM), while its inhibitory eff€ect is markedly (at least 50 ± 100 times) less for myosin light chain kinase (MLCK) or protein kinase C (PKC)[3].
Cell Research Cell lines Human vascular endothelial cells
Concentrations 0.1 to 100 μmol/L
Incubation Time 18 h
Method Human vascular endothelial cells are treated with increasing concentrations of hydroxyfasudil (0.1 to 100 μmol/L) and eNOS expression and activity are measured.
In Vivo
In vivo Intracoronary administration of hydroxyfasudil(HF) causes a significant coronary vasodilation of both small arteries and arterioles in a dose-dependent manner under control conditions with a resultant increase in CBF(coronary blood flow). Intracoronary hydroxyfasudil does not significantly alter mean aortic pressure or heart rate. Pretreatment with hydroxyfasudil markedly reduces the I/R-induced myocardial infarct size, and this beneficial effect of hydroxyfasudil is significantly attenuated by L-NMMA. NO may be involved in those cardiovascular protective effects of hydroxyfasudil. Hydroxyfasudil may also be effective for the treatment of pulmonary hypertension[2]. HF protects the myocardium subjected to pacing-induced ischaemia through the increase in the regional myocardial blood flow[3].
Animal Research Animal Models Mongrel dogs
Dosages 10, 30, and 100 μg/kg
Administration IC(Intracoronary administration)

Chemical Information & Solubility

Molecular Weight 343.83 Formula

C14H17N3O3S·HCl·xH2O

CAS No. 155558-32-0 SDF Download Hydroxyfasudil (HA-1100) HCl SDF
Smiles C1CNCCN(C1)S(=O)(=O)C2=CC=CC3=C2C=CNC3=O.Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 68 mg/mL ( (197.77 mM); Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 60 mg/mL

Ethanol : Insoluble


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy Hydroxyfasudil (HA-1100) HCl | Hydroxyfasudil (HA-1100) HCl supplier | purchase Hydroxyfasudil (HA-1100) HCl | Hydroxyfasudil (HA-1100) HCl cost | Hydroxyfasudil (HA-1100) HCl manufacturer | order Hydroxyfasudil (HA-1100) HCl | Hydroxyfasudil (HA-1100) HCl distributor