CJ-042794 is a potent and selective antagonist of the prostaglandin E₂ (PGE₂) EP₄ receptor, a G-protein-coupled receptor that mediates increases in intracellular cyclic AMP (cAMP) levels. In vitro studies demonstrate that CJ-042794 inhibits [³H]-PGE₂ binding to the human EP₄ receptor with a mean pKᵢ of 8.5, exhibiting at least 200-fold selectivity over other EP receptor subtypes (EP₁, EP₂, and EP₃). It competitively inhibits PGE₂-induced cAMP elevation in HEK293 cells overexpressing the human EP₄ receptor, with a mean pA₂ value of 8.6. Additionally, in human whole blood assays, CJ-042794 reverses the inhibitory effect of PGE₂ on lipopolysaccharide-induced tumor necrosis factor-alpha production in a concentration-dependent manner.
MedKoo Cat#: 513697
Name: CJ-042794
CAS#: 847728-01-2
Chemical Formula: C22H17ClFNO4
Exact Mass: 413.0830
Molecular Weight: 413.83
Elemental Analysis: C, 63.85; H, 4.14; Cl, 8.57; F, 4.59; N, 3.38; O, 15.46
The following data is based on the product molecular weight 413.83 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 |
