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AZD1981
- Soluble in 0.1N NaOH(aq) and DMSO
- MF: C19H17ClN2O3S
- MW: 388.87
Description
AZD1981 is a potent, orally bioavailable and selective CRTh2/DP2 receptor antagonist. It inhibits prostaglandin D2 binding to human CRTh2 with a reported IC50 value of 4 nM.
CRTh2 mediates prostaglandin D2-driven recruitment and activation of Th2 cells, eosinophils and basophils in allergic inflammation. AZD1981 is relevant for asthma, allergic rhinitis and inflammatory airway pharmacology studies.
Key Features
- Potent CRTh2/DP2 antagonist
- Blocks PGD2 binding to human CRTh2
- Orally bioavailable inflammatory receptor antagonist
- Relevant to Th2 and eosinophil biology
Applications
- CRTh2 receptor pharmacology
- Allergic inflammation studies
- Asthma and airway inflammation models
- Prostaglandin D2 signaling assays
More Information
| Parent CAS No. | 802904-66-1 |
|---|---|
| Chemical Name | 2-(4-acetamido-3-(4-chlorophenylthio)-2-methyl-1H-indol-1-yl)acetic acid |
| SMILES | N1(CC(O)=O)C2=C(C(NC(C)=O)=CC=C2)C(SC2=CC=C(Cl)C=C2)=C1C |
| MFCD | N.A. |
| InChi | 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) |
| InChiKey | JWYIGNODXSRKGP-UHFFFAOYSA-N |
| CID | 11292191 |
| Short Description | CRTH2 antagonist |
References
- JA Schmidt et al. Biochemical and pharmacological characterization of AZD1981, an orally available selective DP2 antagonist in clinical development for asthma. Br. J. Pharmacol. 2013, 168(7), 1626-1638.
- N Snell et al. Efficacy and safety of AZD1981, a CRTH2 receptor antagonist, in patients with moderate to severe COPD. Respir Med. 2013 Jul 1. pii: S0954-6111(13)00218-7.
- T Luker et al. Substituted indole-1-acetic acids as potent and selective CRTh2 antagonists-discovery of AZD1981. Bioorg. Med. Chem. Lett. 2011, 21(21), 6288-6292.
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