Cas No.: | 866460-33-5 |
Synonyms: | ACT129968,ACT-129968,ACT 129968 |
SMILES: | O=C(CN1C2C=CC(=CC=2C2CN(CCC1=2)C(=O)C1C=CC=C2C=1C=CC=C2)F)O |
Formula: | C24H19FN2O3 |
M.Wt: | 402.42 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | Setipiprant is an orally available, selective CRTH2 antagonist. CRTH2 is a G protein-coupled receptor for PGD2.IC50 value: 6.0 nM |
Target: | IC50 value: 6.0 nM Target: PGD2 |
In Vitro: | Setipiprant is an orally available, selective CRTH2 (chemoattractant receptor-homologous molecule expressed on T helper [Th]-2 cells) antagonist. CRTH2 is a G protein-coupled receptor for prostaglandin (PGD2). PGD2 is produced by the mast cells and is a key mediator in various inflammatory diseases, including allergy and asthma. Binding of PGD2 to CRTH2, which are expressed on the surface of blood-borne cells, induces chemotaxis of Th2 cells, basophils, and eosinophils, and stimulates cytokine release from these cells. Thus, antagonism of CRTH2 receptors is considered to be a promising therapeutic target for various allergic diseases and asthma. |