Acenocoumarol-d4 is intended for use as an internal standard for the quantification of acenocoumarol by GC- or LC-MS. Acenocoumarol is an anticoagulant and vitamin K antagonist.1 It inhibits the reduction of vitamin K1 epoxide to vitamin K1 by vitamin K1 epoxide reductase (VKOR;IC50 = 1.5 and 5.8 nM for VKORC1 and VKORC1L1, respectively).1 Acenocoumarol also inhibits a variety of VKOR mutants in cell-based reporter assays (IC50s = 0.54-11.21 nM).2 It prolongs prothrombin time in rat blood when administered at a dose of 1.5 mg/kg.3
1.Czogalla, K.J., Liphardt, K., HÖning, K., et al.VKORC1 and VKORC1L1 have distinctly different oral anticoagulant dose-response characteristics and binding sitesBlood Adv.2(6)691-702(2018) 2.Chen, X., Jin, D.-Y., Stafford, D.W., et al.Evaluation of oral anticoagulants with vitamin K epoxide reductase in its native milieuBlood132(18)1974-1984(2018) 3.Meinertz, T., Kasper, W., Kahl, C., et al.Anticoagulant activity of the enantiomers of acenocoumarolBr. J. Clin. Pharmacol.5(2)187-188(1978)