An EP4 receptor antagonist
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E7046

Item No. 19673

Technical Information
Formal Name
4-[(1S)-1-[[[3-(difluoromethyl)-1-methyl-5-[3-(trifluoromethyl)phenoxy]-1H-pyrazol-4-yl]carbonyl]amino]ethyl]-benzoic acid
CAS Number
1369489-71-3
Molecular Formula
C22H18F5N3O4
Formula Weight
Purity
≥98%
Formulation
A crystalline solid
DMF: 2 mg/mlDMSO: 14 mg/mlDMSO:PBS (pH 7.2) (1:5): 0.16 mg/mlEthanol: 12 mg/ml
λmax
234 nm
SMILES
OC(C1=CC=C([C@H](C)NC(C2=C(OC3=CC=CC(C(F)(F)F)=C3)N(C)N=C2C(F)F)=O)C=C1)=O
InChi Code
InChI=1S/C22H18F5N3O4/c1-11(12-6-8-13(9-7-12)21(32)33)28-19(31)16-17(18(23)24)29-30(2)20(16)34-15-5-3-4-14(10-15)22(25,26)27/h3-11,18H,1-2H3,(H,28,31)(H,32,33)/t11-/m0/s1
InChi Key
MKLKAQMPKHNQPR-NSHDSACASA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    E7046 is an antagonist of the prostaglandin E2 (PGE2) receptor subtype EP4 (IC50 = 13.5 nM).1 It inhibits PGE2-induced activation of pro-tumor type 2 macrophages and prevents PGE2-induced suppression of T cell proliferation in isolated human peripheral blood monocytes (PBMCs) when used at concentrations ranging from 0.1 to 3 µM. E7046 (5, 50, and 150 mg/kg) reduces tumor volume in Panc02 murine pancreatic and EMT6 murine breast cancer models.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Albu, D.I., Wang, Z., Huang, K.-C., et alEP4 Antagonism by E7046 diminishes myeloid immunosuppression and synergizes with Treg-reducing IL-2-diphtheria toxin fusion protein in restoring anti-tumor immunity. Oncoimmunology 6(8), e1338239 (2017).