Melagatran

Melagatran is an inhibitor of thrombin (K_i = 0.002 µM) and an active metabolite of the prodrug ximelagatran (Item No. 16862).¹ It is selective for thrombin over a variety of serine proteases (K_is = 0.6-10.2 µM) but also inhibits trypsin (K_i = 0.004 µM). Melagatran inhibits thrombin-induced aggregation of isolated washed human platelets (IC₅₀ = 1.9 nM). It decreases the dry weight of thrombi in rats (ED₅₀ = 16 µg/kg).² Melagatran increases total bleeding time and blood loss in rats (ID₅₀s = 300 and 6.8 µg/kg, respectively).³ Melagatran (5 µmol/kg per hour), alone or in combination with tissue plasminogen activator (tPA), reduces brain infarct volume and increases blood reperfusion in a rat model of ischemia-induced traumatic brain injury (TBI).⁴

WARNING This product is not for human or veterinary use.

1. Gustafsson, D., Antonsson, T., Bylund, R., et al. Effects of melagatran, a new low-molecular-weight thrombin inhibitor, on thrombin and fibrinolytic enzymes. Thromb. Haemost. 79(1), 110-118 (1998).

2. Eriksson, B.I., Carlsson, S., Halvarsson, M., et al. Antithrombotic effect of two low molecular weight thrombin inhibitors and a low-molecular weight heparin in a caval vein thrombosis model in the rat. Thromb. Haemost. 78(5), 1404-1407 (1997).

3. Elg, M., Gustafsson, D., and Carlsson, S. Antithrombotic effects and bleeding time of thrombin inhibitors and warfarin in the rat. Thromb. Res. 94(3), 187-197 (1999).

4. Wang, C.X., Ding, X., and Shuaib, A. Treatment with melagatran alone or in combination with thrombolytic therapy reduced ischemic brain injury. Exp. Neurol. 213(1), 171-175 (2008).