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    Nafamostat Mesylate (FUT175)
    Nafamostat Mesylate (FUT175)

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    This product is for research use only, not for human use. We do not sell to patients.
    Number: - + Pieces(InventoryPieces)
    InvivoChem Cat #: V0707
    CAS #: 82956-11-4Purity ≥98%

    Description: Nafamostat mesylate (formerly also known as FUT-175) is a novel and synthetic serine protease inhibitor, which is used as a short-acting anticoagulant during hemodialysis. Nafamostat promotes endothelium-dependent vasorelaxation via the Akt-eNOS dependent pathway. Nafamostat mesylate can also be used for the treatment of pancreatitis and has antiviral and anti-cancer activity.

    References: Thromb Haemost. 1996 Jan;75(1):76-82; Eur J Pharmacol. 2006 Jan 13;530(1-2):172-8. 

    Related CAS #: 80251-32-7 (HCl)  81525-10-2 (free base)   82956-11-4 (mesylate)

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    • 香港大学
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    Molecular Weight (MW)539.58
    FormulaC19H17N5O2.2CH4O3S
    CAS No.82956-11-4
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 20 mg/mL (37.1 mM)
    Water: 53 mg/mL (98.2 mM)
    Ethanol: <1 mg/mL
    Other info

    Chemical Name: 6-Amidino-2-naphthyl 4-guanidinobenzoate dimethanesulfonate

    InChi Key: SRXKIZXIRHMPFW-UHFFFAOYSA-N

    InChi Code: InChI=1S/C19H17N5O2.2CH4O3S/c20-17(21)14-2-1-13-10-16(8-5-12(13)9-14)26-18(25)11-3-6-15(7-4-11)24-19(22)23;2*1-5(2,3)4/h1-10H,(H3,20,21)(H4,22,23,24);2*1H3,(H,2,3,4)

    SMILES Code: CS(=O)(O)=O.CS(=O)(O)=O.O=C(OC1=CC=C2C=C(C(N)=N)C=CC2=C1)C3=CC=C(NC(N)=N)C=C3

    SynonymsFUT175; Nafamostat mesylate; FUT 175; FUT-175; nafamostat mesilate; .


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    In Vitro

    In vitro activity: 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. 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. 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.


    Cell Assay: 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.

    In VivoNafamostat 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. 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.
    Animal modelFive-week-old male nude mice
    Formulation & Dosage30 μg/g; i.p. injection
    References

    Thromb Haemost. 1996 Jan;75(1):76-82; Eur J Pharmacol. 2006 Jan 13;530(1-2):172-8. 


    These protocols are for reference only. InvivoChem does not independently validate these methods.

     Nafamostat Mesylate Nafamostat Mesylate 
    Effect of mast cell deficiency on the inhibitory action of nafamostat mesilate ...
    Eur J Pharmacol. 2006 Jan 13;530(1-2):172-8.
    Effects of nafamostat mesilate (NFM) and terfenadine (TRF) on plasma ...
    Eur J Pharmacol. 2006 Jan 13;530(1-2):172-8.
    Effect of nafamostat mesilate (NFM) on the activity of tryptase in the skin. The ...
    Eur J Pharmacol. 2006 Jan 13;530(1-2):172-8.
     
    PAR-2 involvement in tryptase- and compound 48/80-induced scratching. (A) ...
    Eur J Pharmacol. 2006 Jan 13;530(1-2):172-8.


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