Nafamostat mesylate Inhibitor CAS No. 82956-11-4

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Cat. No.	Name	Size	Price	Add Cart
KI0766	Nafamostat mesylate	10 mg	$154
KI0766	Nafamostat mesylate	50 mg	$496

Chemical Characteristic

Product Name	Nafamostat mesylate
Synonyms	Futhan, FUT-175
CAS No.	82956-11-4
Molecular Weight	539.58
Formula	C₂₁H₂₅N₅O₈S₂
Chemical Structure

Biological activities

Nafamostat mesylate is a synthetic serine protease inhibitor. Nafamostat has been commonly used as an anticoagulant during continuous renal replacement therapy (CRRT).^[1] Nafamostat mesylate inhibits plasma kallikrein with an IC50 of 3 nM.^[2] Nafamostat mesylate blocks the activity of purified human lung tryptase.^[3] Nafamostat mesylate prevents thrombin (0.5 IU/mL)-induced thromboxane B2 (TXB2) formation with an IC50 of 1.9 µM.^[4] Nafamostat mesylate concentration-dependently inhibits the initial-phase transient component of biphasic acid-sensing ion channels 3 (ASIC3) currents with an IC50 of approximately 2.5 µM.^[5] Nafamostat mesylate prevents tissue factor-F.Vlla complex activity with an IC50 of 0.15 µM.^[6] Nafamostat mesylate suppresses the production of platelet-derived growth factor (PDGF)-BB in the neointima and the medial smooth muscle cell layer.^[7] Pretreatment of nafamostat mesylate (3 or 10 mg/kg) significantly inhibits the ioxaglate-induced vascular hyperpermeability. Pretreatment with nafamostat mesylate at the dose of 10 mg/kg completely reverses the decrease in arterial partial oxygen pressure induced by ioxaglate injection.^[3]

Protocols

In vivo: FUT-175 is dissolved in saline.^[7]

References

[1] Maruyama Y, et al. Nafamostat mesilate as an anticoagulant during continuous veno-venous hemodialysis: a three-year retrospective cohort study. Int J Artif Organs. 2011, 34(7): 571-576. 閵嗏偓閵嗏偓 [2] Hitomi Y, et al. Inhibitory effect of a new synthetic protease inhibitor (FUT-175) on the coagulation system. Haemostasis. 1985, 15(3): 164-168. 閵嗏偓閵嗏偓 [3] Sendo T, et al. A potent tryptase inhibitor nafamostat mesilate dramatically suppressed pulmonary dysfunction induced in rats by a radiographic contrast medium. Br J Pharmacol. 2003, 138(5): 959-967. 閵嗏偓閵嗏偓 [4] Fuse I, et al. Inhibitory mechanism of human platelet aggregation by nafamostat mesilate. Platelets. 1999, 10(4): 212-218. 閵嗏偓閵嗏偓 [5] Ugawa S, et al. Nafamostat mesilate reversibly blocks acid-sensing ion channel currents. Biochem Biophys Res Commun. 2007, 363(1): 203-208. 閵嗏偓閵嗏偓 [6] Uchiba M, et al. Effect of nafamostat mesilate, a synthetic protease inhibitor, on tissue factor-factor VIIa complex activity. Thromb Res. 1994, 74(2): 155-161. 閵嗏偓閵嗏偓 [7] Sawada M, et al. Prevention of neointimal formation by a serine protease inhibitor, FUT-175, after carotid balloon injury in rats. Stroke. 1999, 30(3): 644-650. 閵嗏偓閵嗏偓

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