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Nafamostat Mesylate(FUT-175)Serine protease inhibitor

Nafamostat Mesylate(FUT-175)

Catalog No. A2586
Size Price Stock Qty
10mM (in 1mL DMSO) $55.00 In stock
Evaluation Sample $28.00 In stock
10mg $50.00 In stock
50mg $150.00 In stock

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Sample solution is provided at 25 µL, 10mM.

Quality Control

Quality Control & MSDS

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Chemical structure

Nafamostat Mesylate(FUT-175)

Related Biological Data

Nafamostat Mesylate(FUT-175)

Related Biological Data

Nafamostat Mesylate(FUT-175)

Biological Activity

Description Nafamostat Mesylate is an anticoagulant.
Targets Serine Protease          
IC50            

Protocol

Cell experiment [1]:

Cell lines

The human pancreatic tumor cell lines PANC-1

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months.

Reaction Conditions

3 h; 160 μg/mL

Applications

In assessment of the NF- κB activation by ELISA, concentration of NF- κB p65 in the nuclear extracts of PANC-1 cells in combination group was statistically lower than those in oxaliplatin group (p<0.0001). Like nuclear NF-κB levels, phosphorylated IκBa levels by Western blot analysis in combination group were significantly lower than those in oxaliplatin group (p=0.037). In other words, FUT-175 inhibits oxaliplatin-induced NF- κB activation by suppressing IκBa phosphorylation in vitro.

Animal experiment [1]:

Animal models

Five-week-old male nude mice

Dosage form

30 μg/g; thrice a week for 6 weeks; intraperitoneal injection

Applications

A pancreatic cancer model was established by injection of PANC-1 cells (5×10-6cells) in 200 μM of PBS subcutaneously into the right side of the back of the animals. In vivo, the tumor growth in combination group (oxaliplatin and nafamostat mesilate) was significantly slower than that of oxaliplatin group (p<0.0001). Tumor volume in combination group was significantly smaller than that of oxaliplatin group (p=0.048).

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1] Gocho T, Uwagawa T, Furukawa K, et al. Combination chemotherapy of serine protease inhibitor nafamostat mesilate with oxaliplatin targeting NF-κB activation for pancreatic cancer[J]. Cancer letters, 2013, 333(1): 89-95.

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Chemical Properties

Cas No. 82956-11-4 SDF Download SDF
Synonyms Nafamostat Mesylate,FUT-175,Futhan
Chemical Name (6-carbamimidoylnaphthalen-2-yl) 4-(diaminomethylideneamino)benzoate;methanesulfonic acid
Canonical 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
Formula C19H17N5O2.2CH4O3S M.Wt 539.59
Solubility Soluble in DMSO > 10 mM Storage Store at -20°C
General tips No
Shipping Condition No

Research Update

1. Combination chemotherapy of nafamostat mesylate with gemcitabine for gallbladder cancer targeting nuclear factor-κB activation. J Surg Res. 2013 Sep;184(1):605-12. doi: 10.1016/j.jss.2013.06.003. Epub 2013 Jun 25.
Abstract
In previous studies, nafamostat mesylate inhibited NF-KB activation and induced apoptosis in pancreatic cancer cells. Nafamostat mesylate is to be evaluated for those effects in gallbladder cancer cells pre-treated with gemcitabine.
2. The role of nafamostat mesylate in continuous renal replacement therapy among patients at high risk of bleeding. Ren Fail. 2012;34(3):279-85. doi: 10.3109/0886022X.2011.647293. Epub 2012 Jan 17.
Abstract
Nafamostate prolonged hemofilter lifespan from 10.2 h to 19.8 h without increasing RBC transfusion in CRRT patients at high risk of bleeding.
3. Nafamostat mesylate, a serine protease inhibitor, demonstrates novel antimicrobial properties and effectiveness in Chlamydia-induced arthritis. Arthritis Res Ther. 2012 Jun 20;14(3):R150. doi: 10.1186/ar3886.
Abstract
Nafamostat mesilate is a serine protease inhibitor that exhibits complementaing-modifying effects and anticoagulant properties and has been largely used in Aisa to control inflammation.
5. Nafamostat mesilate for anticoagulation in continuous renal replacement therapy. Int J Artif Organs. 2013 Mar;36(3):208-16. doi: 10.5301/IJAO.5000191. Epub 2013 Feb 13.
Abstract
Nafamostat mesilate, a serine protease inhibitor, has been assessed for efficacy and safety in CRRT patients.

Background

Nafamostat mesylate, previously known as FUT-175, is an inhibitor of serine protease that inhibits a variety of serine proteases, including trypsin and several proteases in the coagulation cascade. Although it was originally developed as an inhibitor of complements, Nafamostat mesylate has been widely used for the treatment of inflammation (such as acute pancreatitis) and disseminated intravascular coagulation (DIC). Nafamostat mesylate exhibits extremely potent inhibition against human tryptase as well as tryptase-catalyzed hydrolysis of Boc-Phe-Ser-Arg-MCA with inhibition constant Kivalue of 95.3 pM. Besides its protease-inhibiting activity, nafamostat mesylate, in a recent study, displayed its antimicrobial activity by dose-dependently inhibiting the proliferation of chlamydial in vitro.

Reference

Robert D Inman and Basil Chiu. Nafamostat mesylate, a serine protease inhibitor, demonstrates novel antimicrobial properties and effectiveness in Chlamydia-induced arthritis. Arthritis Rsearch & Therapy 2012, 13:R150

Shuji Mori, Yoshinori Itoh, Ryoko Shinohata, Toshiaki Sendo, Ryozo Oishi and Masahiro Nishibori. Nafamostat mesilate is an extremely potent inhibitor of human tryptase. J Pharmacol Sci 92, 420-423 (2003)