An EP4 antagonist
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EP4 Antagonist 14

Item No. 38427

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[[[[2-[[4-(trifluoromethyl)phenyl]methyl]-2H-indazol-3-yl]carbonyl]amino]methyl]-benzoic acid
CAS Number
3035217-40-1
Synonyms
  • PGE2 Receptor 4 Antagonist 14
  • Prostaglandin E2 Receptor 4 Antagonist 14
Molecular Formula
C24H18F3N3O3
Formula Weight
453.4
Purity
≥95%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMF: 20 mg/mlDMSO: 20 mg/ml
SMILES
O=C(O)C1=CC=C(CNC(C2=C3C=CC=CC3=NN2CC4=CC=C(C(F)(F)F)C=C4)=O)C=C1
InChi Code
InChI=1S/C24H18F3N3O3/c25-24(26,27)18-11-7-16(8-12-18)14-30-21(19-3-1-2-4-20(19)29-30)22(31)28-13-15-5-9-17(10-6-15)23(32)33/h1-12H,13-14H2,(H,28,31)(H,32,33)
InChi Key
MLXNRQYLAVQFEJ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    10 mg

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    Product 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 & Product Citations
    Product Description References

    1. Cheng, Z., Wang, Y., Zhang, Y., et al. Discovery of 2H-indazole-3-carboxamide derivatives as novel potent prostanoid EP4 receptor antagonists for colorectal cancer immunotherapy. J. Med. Chem. 66(9), 6218-6238 (2023).