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Description: AZD1283 is a novel, potent and selective antagonist of the P2Y12 receptor with EC50 of 3.0 ug/kg/min, TI > 10 and with binding IC50 of 11 nM. In a modified Folts model in dog, AZD1283 dose-dependently induced increases in blood flow and inhibition of ADP-induced platelet aggregation with antithrombotic ED50 values of 3.0 ug/kg/min. The doses that induced a larger than 3-fold increase in bleeding time were 33 ug/kg/min. Thus, the therapeutic index (TI) was >= 10. On the basis of these data, AZD1283 was progressed into human clinical trials as a drug candidate.
References: J Med Chem. 2013 Sep 12; 56(17):7015-24.
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