EP4 Antagonist 14

EP4 antagonist 14 is an antagonist of the prostaglandin E2 (PGE2) receptor subtype EP4 with an IC50 value of 1.1 nM in a reporter assay using HEK293 cells expressing the human receptor. It inhibits PGE2-induced beta-arrestin recruitment in the same cells (IC50 = 0.9 nM). EP4 antagonist 14 (10 µM) decreases PGE2-induced expression of mRNA encoding Il-4, macrophage mannose receptor 1 (Mrc1), chitinase-like protein 3 (Chil3), chemokine (C-X-C) motif ligand 1 (Cxcl1), triggering receptor expressed on myeloid cells 2 (Trem2), and arginase-1 (Arg1), in RAW 264.7 macrophages. In vivo, EP4 antagonist 14 (30 mg/kg per day), in combination with an anti-PD-1 antibody, inhibits tumor growth and increases infiltration of CD8+ T cells into tumors in a CT26 murine colon cancer model.Formal Name: 4-((2-(4-(trifluoromethyl)benzyl)-2H-indazole-3-carboxamido)methyl)benzoic acid. Synonyms: PGE2 Receptor 4 Antagonist 14, Prostaglandin E2 Receptor 4 Antagonist 14. Molecular Formula: C24H18F3N3O3. Formula Weight: 453.4. Purity: >95%. Formulation: (Request formulation change), A solid. Solubility: DMF: 20 mg/ml, DMSO: 20 mg/ml. SMILES: O=C(O)C1=CC=C(CNC(C2=C3C=CC=CC3=NN2CC4=CC=C(C(F)(F)F)C=C4)=O)C=C1. InChi Code: InChI=1S/C24H18F3N3O3/c25-24(26,27)18-11-7-16(8-12-18)14-30-21(19-3-1-2-4-20(19)29-30)22(31)28-13-15-5-9-17(10-6-15)23(32)33/h1-12H,13-14H2,(H,28,31)(H,32,33). InChi Key: MLXNRQYLAVQFEJ-UHFFFAOYSA-N.