Protease-Activated Receptor-1 antagonist 2 is an orally active protease-activated receptor-1 (PAR-1) antagonist, with an IC 50 value of 7 nM. Protease-Activated Receptor-1 antagonist 2 has favorable pharmacokinetic properties which is useful in the research of cardiovascular disease (CVD), such as atherosclerosis and restenosis.