Formulation: A crystalline solid
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
Purity: ≥98%
Formula Markup: C23H21F3N4O3
Formula Weight: 458,4
Shelf life (days): 730
CAS Number: 2287259-07-6
Notes: 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.{58191} 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.
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