• Product NameAZD1283
• Brief DescriptionInhibitors
• Purification99.00%
• Biological ActivityAZD1283 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) 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.
• Target NameP2 Receptor inhibitor
• CAS No. 919351-41-0
• Calculated MW 470.54
• Formulation C23H26N4O5S
• Storage 3 years -20˚C powder;2 years -80˚C in solvent;

• Research Area:cardiovascular system
  SMILES:CCOC(=O)C1=C(N=C(C(=C1)C#N)N2CCC(CC2)C(=O)NS(=O)(=O)CC3=CC=CC=C3)C
  Pathways:Neuroscience
  Receptor:P2Y12
  Boling pt:
  Melting pt:
  Solubility:DMSO:10 mM /mL
  Appearance:
  Remark:For obtaining a higher solubility , please warm the tube at 37 ˚C and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20 ˚C for several month.

1. 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.

• Flow Cytometry (FCM) General Protocol
• Immunofluorescence(IC)
• Immunohistochemistry(Polymer)
• Western Blotting