Name: Fasudil HCl
Brand: Selleck Chemicals
SKU: S1573
Availability: InStock
Rating: 5 (89 reviews)

Jump to

Quality Control

Batch: Purity: 99.99%

99.99

Products Often Used Together with Fasudil HCl

Ozagrel sodium

It and Ozagrel sodium have superior effectiveness over only ozagrel sodium in treating patients at risk of vasospasm after aneurysmal subarachnoid hemorrhage.

Methylcobalamin

It and Methylcobalamin combination therapy improves neuropathic symptoms and nerve conduction velocity in patients with diabetic peripheral neuropathy (DPN).

Related Targets	CDK HSP K-Ras PD-1/PD-L1 Wee1 DNA/RNA Synthesis Microtubule Associated Ras Aurora Kinase Casein Kinase
Other ROCK Products	Y-27632 Dihydrochloride Y-27632 Thiazovivin (TZV) Ripasudil hydrochloride dihydrate NRL-1049 GSK429286A RKI-1447 GSK269962A HCl Y-39983 Dihydrochloride Hydroxyfasudil HCl

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Incubation Time	Activity Description	PMID
U937 cells	Function assay		Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2, IC50=35 μM.	17084087
Sf9 cells	Function assay		Inhibition of His-tagged human MSK1 expressed in Sf9 cells, IC50=5 μM.	10998351
HEK293 cells	Function assay		Inhibition of His-tagged human PRK2 expressed in HEK293 cells, IC50=4 μM.	10998351
Sf9 cells	Function assay		Inhibition of rat ROCK2 expressed in Sf9 cells, IC50=1.9 μM.	10998351
insect cells	Function assay	10 mins	Inhibition of human leukocytic ROCK1 expressed in insect cells using KKRNRTLSV as substrate after 10 mins by pyruvate kinase/lactate dehydrogenase coupled assay, Ki=0.53 μM.	26039570
Sf9 cells	Function assay	90 mins	Inhibition of human recombinant N-terminal his-tagged ROCK1 (3-543) expressed in baculovirus infected Sf9 cells using Biotin-Ahx-AKRRLSSLRA-CONH2 substrate and [gamma-33P]ATP after 90 mins by scintillation proximity assay, IC50=0.3 μM.	17018693
A673	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	29435139
Click to View More Cell Line Experimental Data

Solubility

In vitro
Batch:

Water : 65 mg/mL

DMSO : 57 mg/mL (173.87 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	Saline Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	30.000mg/ml (91.51mM)	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.

In vivo Formulation Calculator (Clear solution)

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

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

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.

Chemical Information, Storage & Stability

Molecular Weight	327.83	Formula	C₁₄H₁₇N₃O₂S.HCl	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	105628-07-7	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	AT-877,HA-1077 HCl			Smiles	C1CNCCN(C1)S(=O)(=O)C2=CC=CC3=C2C=CN=C3.Cl

Mechanism of Action

Targets/IC₅₀/Ki	Rho Calcium channel ROCK2 (Cell-free assay) 330 nM(Ki) PKA (Cell-free assay) 1.6 μM(Ki) PKG (Cell-free assay) 1.6 μM(Ki) PKC (Cell-free assay) 3.3 μM(Ki) MLCK (Cell-free assay) 36 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. Fasudil also exhibits vasodilator actions by inhibition of 5-hydroxytryptamine, noradrenaline, histamine, angiotensin, and dopamine induced spiral strips contraction. Fasudil induces disorganization of actin stress fiber and cell migration inhibition. 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.
Kinase Assay	Cyclic AMP-dependent protein kinase activity assay
Kinase 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.
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. Fasudil administration displays protectable effects on cardiovascular disease and reduces the activation of JNK and attenuates mitochondrial-nuclear translocation of AIF under ischemic injury. 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.
References	[1] https://pubmed.ncbi.nlm.nih.gov/10454191/ [2] https://pubmed.ncbi.nlm.nih.gov/3598899/ [3] https://pubmed.ncbi.nlm.nih.gov/2611484/ [4] https://pubmed.ncbi.nlm.nih.gov/10448094/ [5] https://pubmed.ncbi.nlm.nih.gov/15998434/ [6] https://pubmed.ncbi.nlm.nih.gov/19061880/ [7] https://pubmed.ncbi.nlm.nih.gov/16996142/

Applications

Methods	Biomarkers	PMID
Western blot	ROCK2 / p-ROCK2 / MLC2 / p-MLC2 ABCG2 Moesin / p-Moesin / β-catenin / p-β-catenin	29416017
Immunofluorescence	p-ROCK2 / ABCG2	29416017
Growth inhibition assay	Cell viability	29262624