MF766

MF766 is an antagonist of the prostaglandin E₂ (PGE₂) receptor subtype EP₄ (K_i = 0.23 nM).¹ It is selective for EP₄ over the PGD₂ receptor subtype DP₁ (K_i = 1,648 nM) as well as the EP₁, EP₂, EP₃, and CRTH₂/DP₂ receptors, the PGI₂ receptor (IP), thromboxane receptor (TP), and PGF receptor (FP; K_is = >6,000 nM for all). It inhibits cAMP accumulation induced by PGE₂ (Item No. 14010) in HEK293 cells (IC₅₀ = 1.3 nM). MF766 (312.5 and 1,250 nM) reverses PGE₂-induced decreases in IFN-γ production in IL-2-stimulated primary human natural killer cells.² It reduces paw edema in a rat model of adjuvant-induced arthritis in a dose-dependent manner.¹ MF766 (30 mg/kg) inhibits tumor growth in a CT26 murine colon cancer model.²

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1. Colucci, J., Boyd, M., Berthelette, C., et al. Discovery of 4-{1-[({1-[4-(trifluoromethyl)benzyl]-1H-indol-7-yl}carbonyl)amino]cyclopropyl}benzoic acid (MF-766), a highly potent and selective EP₄ antagonist for treating inflammatory pain. Bioorg. Med. Chem. Lett. 20(12), 3760-3763 (2010).

2. Wang, Y., Cui, L., Georgiev, P., et al. Combination of EP₄ antagonist MF-766 and anti-PD-1 promotes anti-tumor efficacy by modulating both lymphocytes and myeloid cells. Oncoimmunology 10(1), 1896643 (2021).