2. GPCR/G Protein Immunology/Inflammation
  3. Prostaglandin Receptor Interleukin Related
  4. EP4 receptor antagonist 7

EP4 receptor antagonist 7 (Compound 14) is an antagonist of the prostaglandin E2 (PGE2) receptor subtype EP4 with an IC50 value of 1.1 nM. EP4 receptor antagonist 7 inhibits PGE2-induced β-arrestin recruitment in HEK293 cells with an IC50 value of 0.9 nM. EP4 receptor antagonist 7 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. EP4 receptor antagonist 7 combined 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.

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EP4 receptor antagonist 7 Chemical Structure

EP4 receptor antagonist 7 Chemical Structure

CAS No. : 3035217-40-1

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EP4 receptor antagonist 7 Related Antibodies

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Description

EP4 receptor antagonist 7 (Compound 14) is an antagonist of the prostaglandin E2 (PGE2) receptor subtype EP4 with an IC50 value of 1.1 nM. EP4 receptor antagonist 7 inhibits PGE2-induced β-arrestin recruitment in HEK293 cells with an IC50 value of 0.9 nM. EP4 receptor antagonist 7 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. EP4 receptor antagonist 7 combined 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[1].

Molecular Weight

453.41

Formula

C24H18F3N3O3
CAS No.
SMILES

O=C(C1=CC=C(CNC(C2=C3C=CC=CC3=NN2CC4=CC=C(C(F)(F)F)C=C4)=O)C=C1)O
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EP4 receptor antagonist 7 Related Classifications

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Keywords:

EP4 receptor antagonist 73035217-40-1Prostaglandin ReceptorInterleukin RelatedILPGE2β-arrestinHEK293 cellsIL-4Mrc1Chil3Cxcl1Trem2Inhibitorinhibitorinhibit

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