MF766

EP4受体拮抗剂(Ki=0.23nM)；对EP4具有选择性，优于DP1(Ki=1,648nM)，以及EP1、EP2、EP3、CRTH2/DP2、IP、TP和FP受体(所有Kis=>6,000nM)；抑制HEK293细胞中PGE2诱导的cAMP积累(IC50=1.3nM)；逆转312.5和1,250nM时IL-2刺激的原代人类自然杀伤细胞中PGE2诱导的IFN-γ产生减少；减轻佐剂性关节炎大鼠模型中的爪水肿；以30mg/kg的剂量抑制CT26鼠结肠癌模型中的肿瘤生长。An EP4 receptor antagonist (Ki = 0.23 nM); selective for EP4 over DP1 (Ki = 1,648 nM) as well as EP1, EP2, EP3, CRTH2/DP2, IP, TP, and FP recetors (Kis = >6,000 nM for all); inhibits PGE2-induced cAMP accumulation in HEK293 cells (IC50 = 1.3 nM); reverses PGE2-induced decreases in IFN-γ production in IL-2-stimulated primary human natural killer cells at 312.5 and 1,250 nM; reduces paw edema in a rat model of adjuvant-induced arthritis; inhibits tumor growth in a CT26 murine colon cancer model at 30 mg/kg.分子式C27H21F3N2O3分子量478.5O=C(C1=CC=C(C2(CC2)NC(C3=CC=CC4=C3N(CC5=CC=C(C(F)(F)F)C=C5)C=C4)=O)C=C1)O