Nafamostat Mesylate

Catalog No.S1386 Synonyms: FUT-175

Nafamostat Mesylate Chemical Structure

Molecular Weight(MW): 539.58

Nafamostat mesilate is a synthetic serine protease inhibitor, used as an anticoagulant during hemodialysis.

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  • Cancer Lett, 2016, 380(1):87-97.. Nafamostat Mesylate purchased from Selleck.

Purity & Quality Control

Choose Selective Serine Protease Inhibitors

Biological Activity

Description Nafamostat mesilate is a synthetic serine protease inhibitor, used as an anticoagulant during hemodialysis.
Targets
serine protease [1]
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]

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]

Protocol

Solubility (25°C)

In vitro Water 53 mg/mL (98.22 mM)
DMSO 20 mg/mL (37.06 mM)
Ethanol <1 mg/mL
In vivo

* 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.

Chemical Information

Molecular Weight 539.58
Formula

C19H17N5O2.2CH4O3S

CAS No. 82956-11-4
Storage powder
in solvent
Synonyms FUT-175

Bio Calculators

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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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID