AdipoGen Life Sciences

Nafamostat . mesylate

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AG-CR1-3731-M01010 mgCHF 50.00

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Specifications / Handling

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Product Details
Synonyms	Nafamastat; Coahibitor; FUT-175; Futhan; 6-Amidino-2-naphthyl p-guanidinobenzoate dimethanesulfonate
Product Type	Chemical
Properties
Formula	C₁₉H₁₇N₅O₂ . 2CH₄O₃S
MW	347.4 . 192.2
CAS	82956-11-4
RTECS	DG2736000
Purity Chemicals	≥98% (HPLC)
Appearance	White to off-white solid.
Solubility	Soluble in DMSO (25mg/ml) or water (25mg/ml).
Identity	Determined by ¹H-NMR.
InChi Key	SRXKIZXIRHMPFW-UHFFFAOYSA-N
Smiles	NC(C1=CC2=C(C=C1)C=C(OC(C3=CC=C(NC(N)=N)C=C3)=O)C=C2)=N.CS(=O)(O)=O.CS(=O)(O)=O
Shipping and Handling
Shipping	AMBIENT
Short Term Storage	+4°C
Long Term Storage	-20°C
Use/Stability	Stable for at least 2 years after receipt when stored at -20°C.
Documents
MSDS	Download PDF
Product Specification Sheet
Datasheet	Download PDF

Scientific Background Information

Product Description

Nafamostat mesylate is a cell permeable broad spectrum potent and reversible synthetic serine protease inhibitor and kallikrein inhibitor in vitro and in vivo.
It inhibits trypsin (Ki=15nM), tryptase (Ki=95.3pM) and additional proteases in the coagulation cascade including thrombin (Ki=0.84µM).
Nafamostat mesylate is a short-acting anticoagulant with anti-inflammatory, anticancer and antiviral properties.
As a potential anticancer agent, it blocks canonical NF-κB signaling, targets TNFR1-stimulated cleavage of caspase families and the tryptase of mast cells to improve therapeutic outcome and to ameliorate cancer therapy resistance and avoid immune resistance.
It has been shown to reduce eosinophil infiltration, mast cell activation and airway responsiveness in a murine model of asthma.
Inhibits the demethylase activity of the fat mass and obesity-associated protein (FTO).
As antiviral agent, it inhibits Ebola virus, MERS-CoV and SARS-CoV-2 infection in vitro and potentially the spread of COVID-19.
Nafamostat mesylate inhibits TMPRSS2-dependent host cell entry of MERS-CoV. It is also an inhibitor of the enzyme transmembrane serine protease TMPRSS2 and blocks the entry of SARS-CoV-2 (COVID-19) into lung cells in vitro, with roughly 15-fold higher efficiency than Camostat mesylate (Prod. No. AG-CR1-3716), with an EC50 in the low nanomolar range.

Product-specific References

Inhibitory effect of nafamostat mesilate on metastasis into the livers of mice and on invasion of the extracellular matrix by cancer cells: T. Kimura, et al.; J. Int. Med. Res. 20, 343 (1992)
Anticoagulation with nafamostat mesilate, a synthetic protease inhibitor, in hemodialysis patients with a bleeding risk: T. Matsuo, et al.; Haemostasis 23, 135 (1993)
Nafamostat mesilate, a broad spectrum protease inhibitor, modulates platelet, neutrophil and contact activation in simulated extracorporeal circulation: S. Sundaram, et al.; Thromb. Haemost. 75, 76 (1996)
Inhibitory mechanism of human platelet aggregation by nafamostat mesilate: I Fuse, et al.; Platelets 10, 212 (1999)
Nafamostat mesilate, a serine protease inhibitor, suppresses lipopolysaccharide-induced nitric oxide synthesis and apoptosis in cultured human trophoblasts: M. Nakatsuka, et al.; Life Sci. 67, 1243 (2000)
Nafamostat mesilate is an extremely potent inhibitor of human tryptase: S. Mori, et al.; J. Pharmacol. Sci. 92, 420 (2003)
Antitumor effects of Nafamostat mesilate on head and neck squamous cell carcinoma: Y. Yamashita, et al.; Auris Nasus Larynx. 34, 487 (2007)
Nafamostat mesilate, a potent serine protease inhibitor, inhibits airway eosinophilic inflammation and airway epithelial remodeling in a murine model of allergic asthma: M. Ishizaki, et al.; J. Pharmacol. Sci. 108, 355 (2008)
Anti-tumor effect by inhibition of NF-kappaB activation using nafamostat mesilate for pancreatic cancer in a mouse model: K. Furukawa, et al.; Oncol. Rep. 24, 843 (2010)
A Synthetic Serine Protease Inhibitor, Nafamostat Mesilate, Is a Drug Potentially Applicable to the Treatment of Ebola Virus Disease: H. Nishimura & M. Yamaya; Tohoku J. Exp. Med. 237, 45 (2015)
Inhibition of the NF-κB pathway by nafamostat mesilate suppresses colorectal cancer growth and metastasis: Y.X. Lu, et al.; Cancer Lett. 380, 87 (2016)
Identification of Nafamostat as a Potent Inhibitor of Middle East Respiratory Syndrome Coronavirus S Protein-Mediated Membrane Fusion Using the Split-Protein-Based Cell-Cell Fusion Assay: M. Yamamoto, et al.; Antimicrob. Agents Chemother. 60, 6532 (2016)
Nafamostat mesilate, a serine protease inhibitor, suppresses interferon-gamma-induced up-regulation of programmed cell death ligand 1 in human cancer cells: S. Homma, et al.; Int. Immunopharmacol. 54, 39 (2018)
Identification of nafamostat mesilate as an inhibitor of the fat mass and obesity-associated protein (FTO) demethylase activity: X. Han, et al.; Chem. Biol. Interact. 297, 80 (2019)
The Molecular Aspect of Antitumor Effects of Protease Inhibitor Nafamostat Mesylate and Its Role in Potential Clinical Applications: X. Chen, et al.; Front. Oncol. 9, 852 (2019) (Review)
Nafamostat mesylate blocks activation of SARS-CoV-2: New treatment option for COVID-19: M. Hoffmann, et al.; Antimicrob. Agents Chemother. (Epub ahead of print) (2020)

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