DT-678

DT-678 is an orally active antiplatelet and antithrombotic agent. It is a conjugate created by linking the active metabolite of Clopidogrel with 3-nitropyridine-2-thiol through mixed disulfide bonds. Unlike Clopidogrel, DT-678 does not rely on CYP2C19 for activation, directly releasing active substances in vivo through thiol exchange reactions, showing enhanced efficacy. It is applicable for research on acute coronary syndrome and thrombosis.

DT-678, when administered orally at 10 mg/kg as a single dose, inhibits ADP-induced platelet aggregation by 85% in diet-induced obese C57BL/6 mice, with effects lasting 24 hours. In rabbits, a single intravenous dose of DT-678 (0.3-3 mg/kg) reduces FeCl3-induced arterial thrombosis weight in the carotid artery by 42%, 68%, and 81%, respectively. Additionally, a single intravenous dose of 1 mg/kg in rabbits suppresses ADP-induced platelet aggregation by 72% and extends bleeding time by 1.2 times. DT-678, given as a single intravenous bolus dose (0.1-3.0 mg/kg), dose-dependently inhibits ADP-induced platelet activation and aggregation in rabbits without significantly prolonging tongue bleeding time at equivalent antiplatelet doses.