Difethialone is an anticoagulant rodenticide and a vitamin K antagonist.1 It binds to vitamin K epoxide reductase (VKOR; Kis = 0.04 and 0.05 µM for the wild-type and VKORY139F enzyme, respectively). Difethialone is toxic to mice (LD50 = 1.29 mg/kg).2 Formulations containing difethialone have been used in the control of rodent pest populations.
1.Hodroge, A., Longin-Sauvageon, C., Fourel, I., et al.Biochemical characterization of spontaneous mutants of rat VKORC1 involved in the resistance to antivitamin K anticoagulantsArch. Biochem. Biophys.515(1-2)14-20(2011) 2.Vandenbroucke, V., Bousquet-Melou, A., De Backer, P., et al.Pharmacokinetics of eight anticoagulant rodenticides in mice after single oral administrationJ. Vet. Pharmacol. Ther.31(5)437-445(2008)