Nafamostat, also known as FUT-175, is a serine protease inhibitor and an anticoagulant. Nafamostat promotes endothelium-dependent vasorelaxation via the Akt-eNOS dependent pathway. Nafamostat Attenuates Ischemia-Reperfusion-Induced Renal Injury. Nafamostat Attenuates Ischemia-Reperfusion-Induced Renal Injury. Nafamostat protects against acute cerebral ischemia via blood-brain barrier protection. Nafamostat Inhibits TNF-α-Induced Vascular Endothelial Cell Dysfunction by Inhibiting Reactive Oxygen Species Production.

Product information

CAS Number: 82956-11-4

Molecular Weight: 539.58

Formula: C21H25N5O8S2

Synonym:

nafamostat mesilate

FUT-175

FUT 175

FUT175

Related CAS Number:

81525-10-2 (Nafamostat free base)

80251-32-7 (Nafamostat HCl)

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

Smiles: CS(O)(=O)=O.CS(O)(=O)=O.NC(=N)C1=CC2=CC=C(C=C2C=C1)OC(=O)C1C=CC(=CC=1)NC(N)=N

InChiKey: SRXKIZXIRHMPFW-UHFFFAOYSA-N

InChi: 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)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO: 20 mg/mL(37.06 mM). Water: 53 mg/mL(98.22 mM).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

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. 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.

References:

1. Ugawa S, et al. Biochem Biophys Res Commun, 2007, 363(1), 203-208.
2. Uchiba M, et al. Thromb Res, 1994, 74(2), 155-161.
3. Sundaram S, et al. Thromb Haemost, 1996, 75(1), 76-82.

Products are for research use only. Not for human use.