Setipiprant

Description: Setipiprant (ACT-129968) is an orally available, selective CRTH2 antagonist (IC50: 6.0 nM). CRTH2, a G protein-coupled receptor for prostaglandin (PGD2), mediates key inflammatory responses related to allergy and asthma. PGD2, produced by mast cells, binds to CRTH2 on blood-borne cells, inducing chemotaxis of Th2 cells, basophils, and eosinophils, and stimulating cytokine release. Target: Prostaglandin Receptor, GPR. Smiles: C(C(O)=O)N1C2=C(C=3C1=CC=C(F)C3)CN(C(=O)C=4C5=C(C=CC4)C=CC=C5)CC2. References: Diamant Z., et al. Setipiprant, a selective CRTH2 antagonist, reduces allergen-induced airway responses in allergic asthmatics. Clin Exp Allergy. 2014 Aug,44(8):1044-52.