EP4 Receptor Antagonist 1

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 Galpha16. It is selective for EP4 over EP1, EP2, and EP3 receptors (IC50s = >10,000 nM for all). EP4 receptor antagonist 1 inhibits PGE2-induced beta-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.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: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, DMSO:PBS (pH 7.2) (1:6): 0.14 mg/ml. lambdamax: 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.