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AZD1283

CAS No. 919351-41-0

AZD1283( AZD-1283 | AZD1283 | AZD 1283 )

Catalog No. M17661 CAS No. 919351-41-0

AZD1283 is an effective P2Y12 receptor antagonist (EC50: 3.0 ug/kg/min, binding IC50: 11 nM).

Purity : >98% (HPLC)

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Biological Information

  • Product Name
    AZD1283
  • Note
    Research use only, not for human use.
  • Brief Description
    AZD1283 is an effective P2Y12 receptor antagonist (EC50: 3.0 ug/kg/min, binding IC50: 11 nM).
  • Description
    AZD1283 is a potent antagonist of the P2Y12 receptor. In a modified Folts model in dog, both AZD1283 dose-dependently induced increases in blood flow and inhibition of ADP-induced platelet aggregation with antithrombotic ED50 values of 3.0 μg/kg/min. The doses that induced a larger than 3-fold increase in bleeding time were 33 μg/kg/min. Thus, the therapeutic index (TI) was ≥ 10. On the basis of these data, AZD1283 was progressed into human clinical trials as candidate drug.
  • In Vitro
    AZD1283 exhibits excellent antiplatelet aggregation potency with an IC50 value of 3.6 μM.AZD1283 has highly inhibitory activity against CYP450 with IC50 values of 6.62 μM, 0.399 μM and 4.28 μM and 3.64 μM for CYP2C9, CYP2C19, CYP3A4 (Midazolam as the substrate) and CYP3A4 (Testosterone as the substrate), respectively.AZD1283 induces increases in blood flow and inhibition of ADP-induced platelet aggregation with an antithrombotic EC50 value of 3 μg/(kg×min).
  • In Vivo
    AZD1283 exhibits poor liver microsomal stability in rat (T1/2 = 6.08 min), but better in dog microsomes (T1/2 = 201 min) and human microsomes (T1/2 = 65.0 min). Animal Model:Sprague-Dawley rats Dosage:5 mg/kg Administration:p.o.; single dosage Result:Exhibited a Cmax of 25.9 ± 11 ng/mL, a T1/2 of 1.68 ± 0.37 h and a Tmax of 0.25 h.
  • Synonyms
    AZD-1283 | AZD1283 | AZD 1283
  • Pathway
    Angiogenesis
  • Target
    PDE
  • Recptor
    P2Y12
  • Research Area
    Cardiovascular Disease
  • Indication
    ——

Chemical Information

  • CAS Number
    919351-41-0
  • Formula Weight
    470.54
  • Molecular Formula
    C23H26N4O5S
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO : 100 mg/mL. 212.52 mM;H2O : < 0.1 mg/mL
  • SMILES
    CCOC(=O)c1c(nc(c(c1)C#N)N1CCC(CC1)C(=O)NS(=O)(=O)Cc1ccccc1)C
  • Chemical Name
    ethyl 6-(4-((benzylsulfonyl)carbamoyl)piperidin-1-yl)-5-cyano-2-methylnicotinate.

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Bach P,et al. J Med Chem. 2013 Sep 12;56(17):7015-24.
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