TAK-024 is aplateletinhibitor withIC₅₀s of 31, 79 and 51 nM in human, monkey and guinea pig, respectively.

IC50: 31 nM (human platelet), 79 nM (monkey platelet), 51 nM (pig platelet)^[1]

TAK-024 is a platelet inhibitor with IC₅₀s of 31, 79 and 51 nM in human, monkey and guinea pig, respectively. In a preliminary experiment, the IC₅₀value 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 ID₅₀value of TAK-024 onex vivoADP-induced platelet aggregation in guinea pigs is 0.18 μg/kg/min, the dissociation ratio of TAK-024 is found to be 32^[1].

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 ID₅₀value 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^[1].

594.62

C₂₇H₃₄N₁₀O₆

186971-69-7

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.