186971-69-7

IC50: 31 nM (human platelet), 79 nM (monkey platelet), 51 nM (pig platelet)

TAK-024 is a platelet inhibitor with IC ₅₀ s of 31, 79 and 51 nM in human, monkey and guinea pig, respectively. In a preliminary experiment, the IC ₅₀ value of TAK-024 in the heparinized blood sample is 230 nM, 4.5-fold less potent than that in the citrated physiological blood sample. The ID ₅₀ value of TAK-024 on ex vivo ADP-induced platelet aggregation in guinea pigs is 0.18 μg/kg/min, the dissociation ratio of TAK-024 is found to be 32.

Intravenous infusion of TAK-024 (compound 12c) at 1.6 μg/mL/min completely prevents arterial thrombus formation induced by endothelial injury in guinea pigs. Results demonstrate the inhibitory effects of TAK-024 on the carotid thrombosis induced by balloon injury in guinea pigs and the ID ₅₀ value is 0.73 μg/kg/min. A single dose of TAK-024 at 100 μg/kg iv produces almost complete inhibition for 120 min, and about 40% inhibition is observed after 240 min. Dose-dependent inhibition of platelet aggregation is achieved with a single iv dose of 30 to 100 μg/kg of TAK-024.