tcsc3256 AZD1283

AZD1283 is a potent antagonist of the P2Y12 receptor with EC50 of 3.0 ug/kg/min, TI >10; with binding IC50 of 11 nM.

IC50 value: 3.0 ug/kg/min(EC50) [1]

Target: P2Y12 receptor inhibitor

AZD1283 dose-dependently induced increases in blood flow and inhibition of ADP-induced platelet aggregation with antithrombotic ED50 values of 3.0 and 10 μg/kg/min, respectively. The doses that induced a larger than 3-fold

increase in bleeding time were 33 and 100 μg/kg/min for 3 and 13, respectively. Thus, the therapeutic index (TI) was ≥10 for

both compounds. On the basis of these data, compound 3 was progressed into human clinical trials as candidate drug AZD1283.