An EP4 receptor antagonist
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EP4 Receptor Antagonist 1

Item No. 32722

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[(1S)-1-[[[4-(1E)-1-propen-1-yl-1-[[4-(trifluoromethyl)phenyl]methyl]-1H-1,2,3-triazol-5-yl]carbonyl]amino]ethyl]-benzoic acid
CAS Number
2287259-07-6
Molecular Formula
C23H21F3N4O3
Formula Weight
458.4
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlDMSO:PBS (pH 7.2) (1:6): 0.14 mg/ml
λmax
218, 235 nm
SMILES
C[C@@H](C1=CC=C(C=C1)C(O)=O)NC(C2=C(/C=C/C)N=NN2CC3=CC=C(C(F)(F)F)C=C3)=O
InChi Code
InChI=1S/C23H21F3N4O3/c1-3-4-19-20(21(31)27-14(2)16-7-9-17(10-8-16)22(32)33)30(29-28-19)13-15-5-11-18(12-6-15)23(24,25)26/h3-12,14H,13H2,1-2H3,(H,27,31)(H,32,33)/b4-3+/t14-/m0/s1
InChi Key
ZTWUZRMXAVDXJV-XGACYXMMSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    1 mg

    $75

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    5 mg

    $315

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    10 mg

    $589

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    Product Description

    EP4 receptor antagonist 1 is an antagonist of the prostaglandin E2 (PGE2) receptor EP4 that has an IC50 value of 6.1 nM in a calcium flux assay using CHO cells co-expressing the human receptor and Gα16.1 It is selective for EP4 over EP1, EP2, and EP3 receptors (IC50s = >10,000 nM for all). EP4 receptor antagonist 1 inhibits PGE2-induced β-arrestin recruitment in HEK293 cells expressing EP4. It reverses ERK phosphorylation induced by PGE2 in CHO cells expressing EP4 and decreases GM-CSF-induced expression of Il1b, Il4ra, Il6, Arg1, Cox2, and Il10 in RAW 264.7 cells when used at a concentration of 10 µM. EP4 receptor antagonist 1 (50 and 150 mg/kg once per day) reduces tumor volume and increases infiltration of CD8+ T cells into tumors in a murine colon carcinoma model.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Yang, J.-J., Yu, W.-W., Hu, L.-L., et al. Discovery and characterization of 1 H-1,2,3-triazole derivatives as novel prostanoid EP4 receptor antagonists for cancer immunotherapy. J. Med. Chem. 63(2), 569-590 (2020).