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. It is selective for EP4 over EP1, EP2, and EP3 receptors. 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 reduces tumor volume and increases infiltration of CD8+ T cells into tumors in a murine colon carcinoma model.
MedKoo Cat#: 463560
Name: EP4 Receptor Antagonist 1
CAS#: 2287259-07-6
Chemical Formula: C23H21F3N4O3
Exact Mass: 458.1566
Molecular Weight: 458.44
Elemental Analysis: C, 60.26; H, 4.62; F, 12.43; N, 12.22; O, 10.47
The following data is based on the product molecular weight 458.44 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
