Free shipping on all orders over $ 500

Hydroxyfasudil hydrochloride

Cat. No. M5260
Hydroxyfasudil hydrochloride Structure
Synonym:

HA-1100 HCl

Size Price Availability Quantity
5mg USD 90 In stock
10mg USD 133 In stock
50mg USD 520 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control
Biological Activity

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). 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).

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. HF protects the myocardium subjected to pacing-induced ischaemia through the increase in the regional myocardial blood flow.

Protocol
Cell Experiment
Cell lines Human vascular endothelial cells
Preparation 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.
Concentrations 0.1 to 100 μmol/L
Incubation time 18 h
Animal Experiment
Animal models Mongrel dogs
Formulation Physiologic saline
Dosages 10, 30, and 100 μg/kg
Administration IC(Intracoronary administration)
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 343.83
Formula C14H17N3O3S·HCl
CAS Number 155558-32-0
Purity 99.82%
Solubility DMSO: ≥ 30 mg/mL
Storage at -20°C
References

Protective effect of hydroxyfasudil, a Rho kinase inhibitor, on ventral prostatic hyperplasia in the spontaneously hypertensive rat.
Holmström F, et al. Prostate. 2015 Nov;75(15):1774-82. PMID: 26286428.

Effects of the Rho kinase inhibitor, hydroxyfasudil, on bladder dysfunction and inflammation in rats with HCl-induced cystitis.
Shimizu N, et al. Int J Urol. 2013 Nov;20(11):1136-43. PMID: 23419011.

Related ROCK Products
ZINC00881524

ZINC00881524 is a potent and selective ROCK inhibitor.

Ripasudil (K-115) dihydrate

Ripasudil (K-115) hydrochloride dihydrate is potent ROCK inhibitor with IC50 of 51 nM and 19 nM for ROCK1 and ROCK2, respectively, used for the treatment of glaucoma and ocular hypertension.

SR 3677

SR-3677 is a new potent and selective ROCK-II inhibitor with an IC50 of ~3 nM in enzyme and cell based assays; IC50 for ROCK-I is 56 ± 12 nM.

GSK180736A

GSK180736A, developed as a Rho-associated, coiled-coil-containing protein kinase inhibitor, binds to GRK2(G protein-coupled receptor kinase 2) with logIC50 pf -6.6 (logIC50 -4.0 for GRK5 and >-3 for GRK1); ≥400-fold selective for GRK2 over both GRK1 and GRK5.

GSK269962A

GSK269962A is a potent ROCK inhibitor with IC50 values of 1.6 and 4 nM for recombinant human ROCK1 and ROCK2, respectively.

  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Hydroxyfasudil hydrochloride, HA-1100 HCl supplier, ROCK, inhibitors

Contact Us

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.