AZD1283

919351-41-0

C23H26N4O5S

DMSO : 100 mg/mL (212.52 mM; Need ultrasonic); H2O : < 0.1 mg/mL (insoluble)

GPCR/G Protein

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 ug/kg/min, respectively. The doses that induced a larger than 3-fold increase in bleeding time were 33 and 100 ug/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.