产品描述:
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.{72060} It inhibits PGE2-induced β-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.