Gabexate mesylate

Biological Activity

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

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.

Background References

1. FOY: [Ethyl p-(6-guanidinohexanoyloxy) benzoate] methanesulfonate as a serine proteinase inhibitor. I. Inhibition of thrombin and factor Xa in vitro.
   Ohno et al.
   Thromb.Res., 1980;19:579
2. Synthetic inhibitors of trypsin, plasmin, kallikrein, thrombin, C_1r and C₁ esterase.
   Tamura et al.
   Biochim.Biophys.Acta, 1977;484:417
3. 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.
   Yuksel et al.
   J.Pharmacol.Exp.Ther., 2003;305:298
4. 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.
   Ohno et al.
   Thromb.Res., 1981;24:445

Product Datasheets