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AdipoGen Life Sciences
Nafamostat . mesylate
60
CHF
CHF 60.00
In stock
AG-CR1-3731-M01010 mgCHF 60.00
AG-CR1-3731-M05050 mgCHF 180.00
| 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 |
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 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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