Gabexate (mesylate)

Gabexate is a competitive inhibitor of serine proteases that inhibits human thrombin, urokinase, plasmin, and Factor Xa (K_is = 0.97, 1.3, 1.6, and 8.5 μM, respectively).¹,² It also inhibits bovine thrombin, Factor Xa, and trypsin, and porcine plasma kallikrein (K_is = 1.4, 2.1, 2.6, and 0.2 μM, respectively).¹,³ In vitro, gabexate inhibits clotting activity of thrombin (IC₅₀ = 10 μM).¹ In vivo, it inhibits fibrin formation in rats when administered at a continuous infusion of 120 μmol/kg per hour.⁴ Gabexate inhibits LPS-stimulated TNF-α production from monocytes by inhibiting binding of NF-κB and activator protein 1 (AP-1) to target sites and inducing degradation of IκBα.⁵

WARNING This product is not for human or veterinary use.

1. Ohno, H., Kosaki, G., Kambayashi, J., et al. FOY: [ethyl P-(6-guanidinohexanoyloxy) benzoate] methanesulfonate as a serine proteinase inhibitor. I. Inhibition of thrombin and factor Xa in vitro. Thromb. Res. 19(4-5), 579-588 (1980).

2. Menegatti, E., Bolognesi, M., Scalia, S., et al. Gabexate mesylate inhibition of serine proteases: Thermodynamic and computer-graphics analysis. J. Pharm. Sci. 75(12), 1171-1174 (1986).

3. Tamura, Y., Hirado, M., Okamura, K., et al. Synthetic inhibitors of trypsin, plasmin, kallikrein, thrombin, C1r, and C1 esterase. Biochim. Biophys. Acta 484(2), 417-422 (1977).

4. Ohno, H., Kambayashi, J., Chang, S.W., et al. FOY: [ethyl p-(6-guanidinohexanoyloxy) benzoate] methanesulfonate as a serine proteinase inhibitor. II. In vivo effect on coagulofibrinolytic system in comparison with heparin or aprotinin. Thromb. Res. 24(5-6), 445-452 (1981).

5. Yuksel, M., Okajima, K., Uchiba, M., et al. 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(1), 298-305 (2003).