Catalog No.S1386 Synonyms: FUT-175
Molecular Weight(MW): 539.58
Nafamostat mesilate is a synthetic serine protease inhibitor, used as an anticoagulant during hemodialysis.
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|Description||Nafamostat mesilate is a synthetic serine protease inhibitor, used as an anticoagulant during hemodialysis.|
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. 
|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.  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. |
-  Sundaram S, et al. Thromb Haemost, 1996, 75(1), 76-82.
-  Uchiba M, et al. Thromb Res, 1994, 74(2), 155-161.
-  Ugawa S, et al. Biochem Biophys Res Commun, 2007, 363(1), 203-208.
|In vitro||Water||53 mg/mL (98.22 mM)|
|DMSO||20 mg/mL (37.06 mM)|
* 1 mg/ml means slightly soluble or insoluble.
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