For research purposes only

Cat. No BA94673180

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Description of biological activity

Prostaglandin E2 (PGE2) EP4 receptor antagonist. The compound competitively antagonized cAMP accumulation with a pA2 value of 8.7 in HEK293 cells overexpressing rat prostanoid EP4 receptors. Orally administered CJ-042,794 dose-dependently inhibited carrageenan-induced mechanical hyperalgesia with an ED50 value of 4.7 mg/kg (11 μmol/kg) [1]. CJ-042794 inhibited [3H]-PGE2 binding to the human EP4 receptor with a mean pKi of 8.5, a binding affinity that was at least 200-fold more selective for the human EP4 receptor than other human EP receptor subtypes (EP1, EP2, and EP3). CJ-042794 did not exhibit any remarkable binding to 65 additional proteins, including GPCRs, enzymes, and ion channels, suggesting that CJ-042794 is highly selective for the EP4 receptor. PGE2 inhibited the lipopolysaccharide (LPS)-induced production of tumor necrosis factor α (TNFα) in human whole blood (HWB); CJ-042794 reversed the inhibitory effects of PGE2 on LPS-induced TNFα production in a concentration-dependent manner. These results suggest that CJ-042794, a novel, potent, and selective EP4 receptor antagonist, has excellent pharmacological properties that make it a useful tool for exploring the physiological role of EP4 receptors [Life Sciences 2008, 82, 226 – 232].

TECHNICAL INFORMATION

4-({[5-chloro-2-(4-fluorophenoxy)benzoyl] amino}methyl)benzoic acid (CJ-042,794) Prostaglandin E2 (PGE2) EP4 receptor antagonist

IUPAC Name: 4-({[5-chloro-2-(4-fluorophenoxy)benzoyl] amino}methyl)benzoic acid (CJ-042,794)

CAS Number: 847728-01-2

Purity: > 96% chemical purity (LCMS)

1H-NMR spectrum (click to enlarge)

REFERENCES

1. Eur. J. Pharm. 2008, 580, 116-121

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