| Identification | Back Directory | [Name]
EP4 receptor antagonist 7 | [CAS]
3035217-40-1 | [Synonyms]
EP4 receptor antagonist 7
Benzoic acid, 4-[[[[2-[[4-(trifluoromethyl)phenyl]methyl]-2H-indazol-3-yl]carbonyl]amino]methyl]- | [Molecular Formula]
C24H18F3N3O3 | [MOL File]
3035217-40-1.mol | [Molecular Weight]
453.41 |
| Chemical Properties | Back Directory | [Boiling point ]
723.262±60.00 °C(Press: 760.00 Torr)(predicted) | [density ]
1.371±0.14 g/cm3(Temp: 25 °C; Press: 760 Torr)(predicted) | [solubility ]
DMF: 20 mg/ml
DMSO: 20 mg/ml | [pka]
4.197±0.10(predicted) |
| Hazard Information | Back Directory | [Description]
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.1 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.WARNING This product is not for human or veterinary use. | [References]
[1] ZHIYUAN CHENG, WEIQIANG LU* Discovery of 2H-Indazole-3-carboxamide Derivatives as Novel Potent Prostanoid EP4 Receptor Antagonists for Colorectal Cancer Immunotherapy[J]. Journal of Medicinal Chemistry, 2023, 66 9: 6218-6238. DOI: 10.1021/acs.jmedchem.2c02058 |
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