Elinogrel

Elinogrel (PRT060128) is an orally active, selective, competitive, and reversible direct-acting platelet P2Y₁₂ antagonist (IC₅₀ = 20 nM). Elinogrel blocks ADP-induced signaling by directly and reversibly competing for binding to the platelet P2Y₁₂ receptor. Elinogrel exhibits rapid and potent anti-platelet aggregation and antithrombotic activities. Elinogrel is suitable for research into acute coronary syndrome and antithrombotic^[1][2][3][4]. IC50 & Target:IC50: 20 nM (P2Y₁₂)^[2] In Vitro:Elinogrel (PRT060128) (30 μM; 20 min) serves to define and distinguish P2Y₁₂-specific binding sites in mouse and human platelets (platelet-rich plasma or washed platelets)^[2].
Elinogrel exhibits high affinity for the P2Y₁₂ receptor (K_i = 23 nM) and possesses anti-platelet aggregation activity (IC₅₀ = 2.81 μM)^[4]. In Vivo:Elinogrel (PRT060128) (60 mg/kg; p.o.; twice daily; for 3 days; 40-minute post-injury observation) inhibits thrombus formation in a 10% FeCl3 (HY-Y0266)-induced mesenteric artery thrombosis model in wild-type C57BL/6J mice^[2].
Elinogrel (1 mg/kg; i.v.; single dose; 15-minute observation) abolishes residual thrombus formation in an FeCl3-induced thrombosis model in wild-type C57BL/6J mice pretreated with Clopidogrel (HY-15283) (50 mg/kg; oral; for 3 days)^[2].