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Submit ReviewGabexate mesylate
Description: Serine protease inhibitor; inhibits thrombin, trypsin, kallikrein and plasmin
Alternative Names: FOY
Chemical Name: 4-[[6-[(Aminoiminomethyl)amino]-1-oxohexyl]oxy]-benzoic acid ethyl ester mesylate
Purity: ≥98% (HPLC)
Biological Activity for Gabexate mesylate
Gabexate mesylate is a serine protease inhibitor; Gabexate mesylate inhibits trypsin, plasmin, plasma kallikrein and thrombin (IC50 values are 9.4, 30, 41 and 110 μM respectively). Antithrombotic in vitro and in vivo. Gabexate mesylate also inhibits LPS-induced TNF-α production, probably by inhibiting NF-κB and AP-1 activation. Gabexate mesylate attenuates allergen-induced airway inflammation and eosinophils infiltration in the lung of asthma murine model.
Technical Data for Gabexate mesylate
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for Gabexate mesylate
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 41.75 | 100 |
Preparing Stock Solutions for Gabexate mesylate
The following data is based on the product molecular weight 417.48. Batch specific molecular weights may vary from batch to batch due to the degree 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 for Gabexate mesylate
References for Gabexate mesylate
References are publications that support the biological activity of the product.
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 he. or apro. 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
Chen et al (2006) Serine protease inhibitors nafamostat mesilate and gabexate mesilate attenuate allergen induced airway inflammation and eosinophilia in a murine model of asthma. J.Allergy Clin.Immunol. 118 105 PMID: 16815145
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