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Chemical Structure| 802904-66-1 Chemical Structure| 802904-66-1

Structure of AZD1981
CAS No.: 802904-66-1

Chemical Structure| 802904-66-1

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AZD1981 is a potent and selective CRTh2 antagonist and displaces radio-labelled PGD2 from human recombinant DP2 with high potency (pIC50 = 8.4).

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Product Details of AZD1981

CAS No. :802904-66-1
Formula : C19H17ClN2O3S
M.W : 388.87
SMILES Code : O=C(O)CN1C(C)=C(SC2=CC=C(Cl)C=C2)C3=C1C=CC=C3NC(C)=O
MDL No. :MFCD26936340
InChI Key :JWYIGNODXSRKGP-UHFFFAOYSA-N
Pubchem ID :11292191

Safety of AZD1981

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

Description
AZD1981 is a powerful and selective antagonist of CRTh2, effectively competing with radio-labelled PGD2 for binding to the human DP2 receptor, exhibiting a high level of potency (pIC50 = 8.4)[1].
Target
  • GPR

    CRTh2 (DP2) receptor, IC50:4 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
human basophils 1 μM 10 min Evaluate the effect of AZD1981 on basophil shape change, results showed AZD1981 significantly inhibited PGD2-induced shape change Br J Pharmacol. 2013 Apr;168(7):1626-38
human eosinophils 1 µM Evaluate the binding activity of AZD1981 to human recombinant DP2 receptor, results showed AZD1981 effectively displaced [3H]PGD2 binding with pIC50 of 8.4 Br J Pharmacol. 2013 Apr;168(7):1626-38

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Guinea pig Isolated perfused hind limb model Perfusion 10 nM and 100 nM Single dose, lasting 20 to 40 minutes Evaluate the effect of AZD1981 on eosinophil release from guinea pig bone marrow, results showed AZD1981 significantly inhibited DK-PGD2-induced eosinophil release Br J Pharmacol. 2013 Apr;168(7):1626-38

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT01058447 Healthy PHASE1 COMPLETED 2025-03-10 -

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.57mL

0.51mL

0.26mL

12.86mL

2.57mL

1.29mL

25.72mL

5.14mL

2.57mL

References

 

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