Fasudil HCl

Catalog No.S1573 Batch:S157315

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Technical Data

Formula

C14H17N3O2S.HCl

Molecular Weight 327.83 CAS No. 105628-07-7
Solubility (25°C)* In vitro DMSO 66 mg/mL (201.32 mM)
Water 66 mg/mL (201.32 mM)
Ethanol Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
Saline
30.0mg/ml Taking the 1 mL working solution as an example, add 30 mg of this product to 1 ml of physiological saline (0.9% NaCL solution), mix evenly to make it clear, The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description Fasudil HCl, a potent and selective inhibitor of Rho kinase, displays less potent inhibiton over PKA, PKG, PKC and MLCK with Ki of 1.6, 1.6, 3.3, and 36 μM in cell-free assays, respectively. Fasudil is also a calcium channel blocker.
Targets
Rho [1] Calcium channel [2] ROCK2 [1]
(Cell-free assay)
PKA [1]
(Cell-free assay)
PKG [1]
(Cell-free assay)
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330 nM(Ki) 1.6 μM(Ki) 1.6 μM(Ki)
In vitro

Fasudil is a class of calcium antagonists. Fasudil produces a competitive inhibition of the Ca2+-induced contraction of the depolarized rabbit aorta. Fasudil is able to inhibit contractile responses to KCl, phenylephnne (PHE) and prostaglandin (PG) F2a. [2]

Fasudil also exhibits vasodilator actions by inhibition of 5-hydroxytryptamine, noradrenaline, histamine, angiotensin, and dopamine induced spiral strips contraction. [3]

Fasudil induces disorganization of actin stress fiber and cell migration inhibition. [4]

Fasudil inhibits hepatic stellate cells spreading, the formation of stress fibers, and expression of α-SMA with concomitant suppression of cell growth, but does not induce apoptosis. Fasudil suppresses the LPA-induced phosphorylation of ERK1/2, JNK and p38 MAPK. [5]

In vivo

Intra-coronary injection of Fasudil to dogs (30 μg i.a.) produces an approximate 50% increase in CBF. Fasudil (0.01, 0.03, 0.1 and 0.3 mg/kg, bolus, i.v.) dose-dependently decreases MBP and increases HR, VBF, CBF, RBF, and FBF. A total dose of 1.0 ng/mL Fasudil increases cardiac output. The infusion of Fasudil i.v. produces a significant fall in MBP, left ventricular systolic pressure and total peripheral resistance with an increase in HR and cardiac output, but without significant changes in right atrial pressure, dP/dt or left ventricular minute work in dogs. [3]

Fasudil administration displays protectable effects on cardiovascular disease and reduces the activation of JNK and attenuates mitochondrial-nuclear translocation of AIF under ischemic injury. [6]

The oral administration of Fasudil (a dosage of 100 mg/kg/day) significantly reduces incidence and mean maximum clinical score of EAE in SJL/J mice immunized with PLP p139-151. Treatment of mice with Fasudil suppresses the proliferative response of splenocytes to the antigen. Oral administration of Fasudil decreases inflammation, demyelination, axonal loss and APP positivein spinal cord of Fasudil-treated mice. [7]

Protocol (from reference)

Kinase Assay:

[1]

  • Cyclic AMP-dependent protein kinase activity assay

    Cyclic AMP-dependent protein kinase activity is assayed in a reaction mixture containing, in a final volume of 0.2 mL, 50 mM Tris-HCl (pH 7.0), 10 mM magnesium acetate, 2 mM EGTA, 1 μM cyclic AMP or absence of cyclic AMP, 3.3 to 20 μM [r-32P] ATP (4×105 c.p.m.), 0.5 μg of the enzyme, 100 μg of histone H2B and compound. The mixture is incubated at 30 ℃ for 5 min. The reaction is terminated by adding 1mL of ice-cold 20% trichloroacetic acid after adding 500 μg of bovine serum albumin as a carrier protein. The sample is centrifuged at 3000 r.p.m. for 15min, the pellet is resuspended in ice-cold 10% trichloro-acetic acid solution and the centrifugation-resuspension cycle is repeated three times. The final pellet is dissolved in 1 mL of 1 N NaOH and radioactivity is measured with a liquid scintillation counter.

Animal Study:

[3]

  • Animal Models

    Mongrel dogs

  • Dosages

    0.01, 0.03, 0.1 and 0.3 mg/kg

  • Administration

    i.v.

Customer Product Validation

Data from [J Clin Invest, 2014, 124(4), 1646-59]

Data from [Data independently produced by J Clin Invest, 2014, 124(9), 3757-66]

Data from [Data independently produced by Diabetes, 2013, 62(5), 1697-708]

Data from [Data independently produced by , , Pulm Pharmacol Ther, 2018, 50:111-122]

Selleck's Fasudil HCl has been cited by 80 publications

Fasudil may alleviate alcohol-induced astrocyte damage by modifying lipid metabolism, as determined by metabonomics analysis [ PeerJ, 2023, 11:e15494] PubMed: 37304877
Inhibition of the Rho/ROCK pathway promotes the expression of developmental and migration-related genes in astrocytes exposed to alcohol [ Alcohol, 2023, 115:5-12] PubMed: 37481044
A rare non-coding enhancer variant in SCN5A contributes to the high prevalence of Brugada syndrome in Thailand [ medRxiv, 2023, 10.1101/2023.12.19.23299785] PubMed: none
Acquired temozolomide resistance in MGMTlow gliomas is associated with regulation of homologous recombination repair by ROCK2 [ Cell Death Dis, 2022, 13(2):138] PubMed: 35145081
Rho-Kinase Inhibition Improves the Outcome of Focal Subcortical White Matter Lesions [ Stroke, 2022, 53(7):2369-2376] PubMed: 35656825
Arolein, an endogenous aldehyde induces synaptic dysfunction in vitro and in vivo: Involvement of RhoA/ROCK2 pathway [ Aging Cell, 2022, e13587] PubMed: 35315217
AURKA and PLK1 inhibition selectively and synergistically block cell cycle progression in diffuse midline glioma [ iScience, 2022, 25(6):104398] PubMed: 35637734
Amyloid-β Induces Cdh1-Mediated Rock2 Stabilization Causing Neurodegeneration [ Front Pharmacol, 2022, 13:884470] PubMed: 35496276
Involvement of Paired Immunoglobulin-Like Receptor B in Cognitive Dysfunction Through Hippocampal-Dependent Synaptic Plasticity Impairments in Mice Subjected to Chronic Sleep Restriction [ Mol Neurobiol, 2022, 10.1007/s12035-022-03127-4] PubMed: 36417104
Establishment and characterization of immortalized sweat gland myoepithelial cells [ Sci Rep, 2022, 12(1):7] PubMed: 34997030

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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