Biological Activity
Serine protease inhibitor; inhibits trypsin, plasmin, plasma kallikrein and thrombin (IC50 values are 9.4, 30, 41 and 110 μM respectively). Antithrombotic in vitro and in vivo. Also inhibits LPS-induced TNF-α production, probably by inhibiting NF-κB and AP-1 activation.
Technical Data
| M. Wt | 417.48 |
| Formula | C16H23N3O4.CH3SO3H |
| Storage | Desiccate at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 56974-61-9 |
| PubChem ID | 6604915 |
| InChI Key | ICDMLAQPOAVWNH-HAAQQRBASA-N |
| Smiles | CS(O)(=O)=O.CCOC(=O)C1=CC=C(OC(=O)CCCCCNC(N)=N)C=C1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| phosphate buffered saline | 20.87 | 50 | |
| water | 41.75 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 417.48. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.4 mL | 11.98 mL | 23.95 mL |
| 5 mM | 0.48 mL | 2.4 mL | 4.79 mL |
| 10 mM | 0.24 mL | 1.2 mL | 2.4 mL |
| 50 mM | 0.05 mL | 0.24 mL | 0.48 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Ohno et al (1980) FOY: [Ethyl p-(6-guanidinohexanoyloxy) benzoate] methanesulfonate as a serine proteinase inhibitor. I. Inhibition of thrombin and factor Xa in vitro. Thromb.Res. 19 579 PMID: 6449757
Ohno et al (1981) FOY: [Ethyl p-(6-guanidinohexanoyloxy) benzoate] methanesulfonate as a serine proteinase inhibitor. II. In vivo effect on coagulo-fibrinolytic system in comparison with heparin or aprotinin. Thromb.Res. 24 445 PMID: 6178174
Tamura et al (1977) Synthetic inhibitors of trypsin, plasmin, kallikrein, thrombin, C1r and C1 esterase. Biochim.Biophys.Acta 484 417 PMID: 143965
Yuksel et al (2003) Gabexate mesilate, a synthetic protease inhibitor, inhibits lipopolysaccharide-induced tumor necrosis factor-α production by inhibiting activation of both nuclear factor-κB and activator protein-1 in human monocytes. J.Pharmacol.Exp.Ther. 305 298 PMID: 12649382
Keywords: Gabexate mesylate, supplier, Serine, protease, inhibits, inhibitors, thrombin, trypsin, kallikrein, plasmin, TNF-α, TNF-alpha, production, antithrombotic, agent, Proteases, Proteinases, Interleukins, Tumor, Necrosis, Factor-α, Factor-alpha, Cytokines, PAR, Receptors, Protease-Activated, proteinase, FOY, Protease-Activated, Receptors, Cytokines, Other, Proteases, Protease-Activated, Receptors, Tocris Bioscience
