Home Proteases Serine Protease inhibitor - COVID-19 inhibitor - Apoptosis related inhibitor - SARS-CoV inhibitor Nafamostat mesilate (FUT-175) For research use only.

Nafamostat mesilate (FUT-175)

Nafamostat mesilate is a synthetic serine protease inhibitor, used as an anticoagulant during hemodialysis. Nafamostat mesylate blocks activation of SARS-CoV-2 and is investigated as a new treatment option for COVID-19. Nafamostat Mesilate attenuates inflammation and apoptosis.

Nafamostat mesilate (FUT-175) Chemical Structure

Nafamostat mesilate (FUT-175) Chemical Structure

CAS No. 82956-11-4

Purity & Quality Control

Nafamostat mesilate (FUT-175) Related Products

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
NS0 Function assay 15 mins Inhibition of recombinant C-terminal His10-tagged human Hepsin (R45 to L17 residues) D161E/ R162K double mutant expressed in mouse NS0 cells using Boc-QRR-AMC as substrate after 15 mins by automated fluorescence assay, IC50=0.005μM. 29701962
Sf9 Function assay 30 mins Inhibition of recombinant N-terminal His-tagged HGFA (unknown origin) expressed in baculovirus-infected Sf9 cells using Boc-QLR-AMC as substrate incubated for 30 mins prior to substrate addition by fluorescence assay, Ki=0.025μM. 25882520
Sf9 Function assay 30 mins Inhibition of recombinant N-terminal His-tagged HGFA (unknown origin) expressed in baculovirus-infected Sf9 cells incubated for 30 mins prior to cromogenic substrate addition by spectrophotometry, IC50=0.15μM. 25882520
MDA-MB-231 Function assay 15 mins Inhibition of HGFA in human MDA-MB-231 cells assessed as inhibition of c-MET phosphorylation after 15 mins by immunoblotting, EC50=0.49μM. 25408834
Click to View More Cell Line Experimental Data

Biological Activity

Description Nafamostat mesilate is a synthetic serine protease inhibitor, used as an anticoagulant during hemodialysis. Nafamostat mesylate blocks activation of SARS-CoV-2 and is investigated as a new treatment option for COVID-19. Nafamostat Mesilate attenuates inflammation and apoptosis.
Targets
serine protease [1]
In vitro
In vitro

Nafamostat mesilate significantly inhibits the release of platelet beta-thromboglobulin (beta TG) at 60 and 120 min. Nafamostat mesilate (NM) prevents any significant release of neutrophil elastase; at 120 min, plasma elastase-alpha 1-antitrypsin complex is 0.16 mg/mL in the NM group and 1.24 mg/mL in the control group. Nafamostat mesilate completely inhibits formation of complexes of C1 inhibitor with kallikrein and FXIIa. [1]

Nafamostat mesilate inhibits several proteases which may be importantly involved in the pathophysiology of disseminated intravascular coagulation (DIC).Nafamostat mesilate inhibits extrinsic pathway activity (TF-F.VIIa mediated-F.Xa generation) in a concentration dependent manner with IC50 of 0.1 μM. [2]

Nafamostat mesilate produces concentration-dependent inhibition of the initial-phase transient component of biphasic ASIC3 currents with an IC50 value of approximately 2.5 mM. [3]
Cell Research Cell lines NCM460 cells
Concentrations 5 μM
Incubation Time 24 h
Method

Cells were treated with indicated concentration of drug for 24 h.
In Vivo
In vivo

Nafamostat mesilate (10 mg/kg) inhibits scratching induced by tryptase but not by histamine and serotonin. Nafamostat mesilate (1-10 mg/kg) produces the dose-dependent inhibition of scratching induced by intradermal compound 48/80 (10 mg/site). Nafamostat mesilate (10 mg/kg) suppresses tryptase activity in the mouse skin. [4]

Nafamostat mesilate inhibits gemcitabine-induced NF-kappaB activation, enhances apoptosis by gemcitabine and suppresses pancreatic tumor growth. Nafamostat mesilate combined with Gemcitabine improves the body weight loss of mice induced by Gemicitabine. [5]
Animal Research Animal Models Male ICR-SCID nude mice
Dosages 30 mg/kg
Administration i.p.

Chemical Information & Solubility

Molecular Weight 539.58 Formula

C19H17N5O2.2CH4O3S
CAS No. 82956-11-4 SDF Download Nafamostat mesilate (FUT-175) SDF
Smiles CS(=O)(=O)O.CS(=O)(=O)O.C1=CC(=CC=C1C(=O)OC2=CC3=C(C=C2)C=C(C=C3)C(=N)N)N=C(N)N
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (185.32 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 100 mg/mL

Ethanol : Insoluble


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In vivo
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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.

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