AZD1283

Description: AZD1283 is an effective P2Y12 receptor antagonist (EC50: 3.0 ug/kg/min, binding IC50: 11 nM). 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 induced the increase in bleeding time at 33 and 100 µg/kg/min for 3- and 13-fold, respectively. Thus, the therapeutic index (TI) was >10 for both compounds. Target: P2Y Receptor. Smiles: CCOC(=O)c1cc(C#N)c(nc1C)N1CCC(CC1)C(=O)NS(=O)(=O)Cc1ccccc1. References: Bach P,et al. Lead optimization of ethyl 6-aminonicotinate acyl sulfonamides as antagonists of the P2Y12 receptor. separation of the antithrombotic effect and bleeding for candidate drug AZD1283. J Med Chem. 2013 Sep 12,56(17):7015-24.