A DP2/CRTH2 receptor antagonist
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AZD 1981

Item No. 20763

Technical Information
Formal Name
4-(acetylamino)-3-[(4-chlorophenyl)thio]-2-methyl-1H-indole-1-acetic acid
CAS Number
802904-66-1
Molecular Formula
C19H17ClN2O3S
Formula Weight
Purity
≥98%
Formulation
A crystalline solid
DMF: 15 mg/mlDMSO: 15 mg/mlDMSO:PBS (pH 7.2)(1:5): 0.16 mg/ml
λmax
223, 291 nm
SMILES
CC(NC1=C(C(SC2=CC=C(Cl)C=C2)=C(C)N3CC(O)=O)C3=CC=C1)=O
InChi Code
InChI=1S/C19H17ClN2O3S/c1-11-19(26-14-8-6-13(20)7-9-14)18-15(21-12(2)23)4-3-5-16(18)22(11)10-17(24)25/h3-9H,10H2,1-2H3,(H,21,23)(H,24,25)
InChi Key
JWYIGNODXSRKGP-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    AZD 1981 is a DP2/CRTH2 receptor antagonist (IC50 = 3.98 nM).1 It is selective for DP2 over a panel of receptors, ion channels, transporters, and enzymes, including DP1, COX-1, and COX-2, at 10 µM. AZD 1981 (3-100 nM) inhibits increases in the expression of CD11b, a cell adhesion molecule, induced by 13,14-dihydro-15-keto-prostaglandin D2 (13,14-dihydro-15-keto-PGD2; Item No. 12610) in isolated human eosinophils. It also inhibits 13,14-dihydro-15-keto-PGD2-induced chemotaxis of isolated human eosinophils and T cells in a concentration-dependent manner.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Schmidt, J.A., Bell, F.M., Akam, E., et alBiochemical and pharmacological characterization of AZD1981, an orally available selective DP2 antagonist in clinical development for asthma. Br. J. Pharmacol. 168(7), 1626-1638 (2013).