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Timapiprant
- OC000459
- Soluble in 0.1N NaOH(aq) and DMSO
- MF: C21H17FN2O2
- MW: 348.37
Description
Timapiprant is a potent, oral and selective CRTH2/DP2 receptor antagonist targeting prostaglandin D2-dependent inflammatory signaling.
CRTH2 is expressed on Th2 cells, eosinophils and basophils and mediates chemotaxis and activation downstream of prostaglandin D2. Timapiprant is used to study allergic inflammation, asthma-related pathways and CRTH2 receptor pharmacology.
Key Features
- Selective CRTH2/DP2 antagonist
- Orally active prostaglandin D2 receptor pathway inhibitor
- Targets Th2 and eosinophil recruitment signaling
- Clinically relevant allergy and asthma research compound
Applications
- CRTH2 receptor binding and functional assays
- PGD2-mediated chemotaxis studies
- Asthma and allergic inflammation models
- Th2/eosinophil pathway research
More Information
| Parent CAS No. | 851723-84-7 |
|---|---|
| Chemical Name | 2-(5-fluoro-2-methyl-3-(quinolin-2-ylmethyl)-1H-indol-1-yl)acetic acid |
| SMILES | N1(CC(O)=O)C2=CC=C(C=C2C(CC2=CC=C3C(C=CC=C3)=N2)=C1C)F |
| MFCD | MFCD18633254 |
| InChi | InChI=1S/C21H17FN2O2/c1-13-17(11-16-8-6-14-4-2-3-5-19(14)23-16)18-10-15(22)7-9-20(18)24(13)12-21(25)26/h2-10H,11-12H2,1H3,(H,25,26) |
| InChiKey | FATGTHLOZSXOBC-UHFFFAOYSA-N |
| CID | 11462174 |
| Short Description | CRTH2 antagonist |
References
- R Pettipher et al. Pharmacologic Profile of OC000459, a Potent, Selective, and Orally Active D Prostanoid Receptor 2 Antagonist That Inhibits Mast Cell-Dependent Activation of T Helper 2 (...). J. Pharmacol. Exp. Ther. 2012, 340(2), 473-482.
- F Horak et al. The CRTH2 antagonist OC000459 reduces nasal and ocular symptoms in allergic subjects exposed to grass pollen, a randomised, placebo-controlled, double-blind trial. Allergy 2012
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