The present invention discloses three materials such as warfarin-4-O-acetyl-Arg-Gly-Asp-Val, warfarin-4-O-acetyl-Arg-Gly-Asp-Ser and warfarin-4-O-acetyl-Arg-Gly-Asp-Phe, preparation methods, anti-arterial thrombus activities, anti-venous thrombosis activities, in vivo vitamin K content lowering activities, in vivo blood coagulation factor II content lowering activities, platelet aggregation inhibition activities thereof, and in vivo platelet membrane glycoprotein IIb / IIIa (GPIIb / IIIa) content lowering activities thereof, and discloses the advantages of no warfarin-like bleeding risk in warfarin-4-O-acetyl-Arg-Gly-Asp-Val, warfarin-4-O-acetyl-Arg-Gly-Asp-Ser and warfarin-4-O-acetyl-Arg-Gly-Asp-Phe, such that the invention discloses applications of warfarin-4-O-acetyl-Arg-Gly-Asp-Val, warfarin-4-O-acetyl-Arg-Gly-Asp-Ser and warfarin-4-O-acetyl-Arg-Gly-Asp-Phe in preparation of anti-arterial thrombus drugs, anti-venous thrombosis drugs, platelet aggregation inhibition drugs, GPIIb / IIIa antagonists, vitamin K antagonists, and blood coagulation factor II antagonists.