ONO-7684

ONO-7684 (ONO-5450598) potently and selectively inhibits activated human coagulation factor XIa with a K_i value of 2 nM, while it exhibits only extremely weak or no inhibitory activity against other tested human coagulation and fibrinolytic enzymes^[2].
ONO-7684 (0.46-0.8 μM) doubles APTT in human, monkey and rabbit plasma, but exerts no effect on PT at concentrations up to 33 μM^[2].
ONO-7684 exhibits detectable bidirectional permeability in human Caco-2 cells, with a flux of 2.5 × 10^-6 cm/sec in the A-to-B direction and 36 × 10^-6 cm/sec in the B-to-A direction^[2].
ONO-7684 exhibits detectable bidirectional permeability in the human colorectal cancer cell line Caco-2 within this experimental system, with a flux of 8.2 × 10^-6 cm/sec in the A→B direction and 28 × 10^-6 cm/sec in the B→A direction^[2].
ONO-7684 (0.5-1.2 μM) doubles the activated partial thromboplastin time (APTT) in human plasma^[2].