CJ-42794

CJ-42794 (CJ-042794) is a potent, orally active, selective prostaglandin E receptor 4 (EP4) antagonist with an IC₅₀ value of 10 nM, which is 200-fold more selective than EP1, EP2 and EP3. CJ-42794 can be used in research of gastric ulcers^[1][2]. IC50 & Target:IC50: 10 nM (EP4)^[1] In Vitro: CJ-042794 (CJ-042794, 0.3-5000 nM; 10 min; hEP4/HEK293 cells) inhibits the PGE₂-induced elevation of cAMP in a concentration-dependent manner with a pIC₅₀ value of 7.5^[1].
CJ-042794 (3-3000 nM; 24 h) reverses the inhibitory effects of PGE₂ (10 nM) on the LPS-induced TNFα production in human whole blood (HWB) in a concentration-dependent manner with a pIC50 value of 6.4^[1].
In Vivo: CJ-042794 (CJ-042794; 0.3-3 mg/kg; i.d.; once) antagonizes the HCO3 stimulatory action of AE1-329 in the duodenum^[1].
CJ-042794 (30 and 50 mg/kg; p.o.; once) does not cause any damage to the gastric mucosa of normal rats and has no gastric ulcerogenic response to cold-restraint stress^[1].
CJ-042794 (30 and 50 mg/kg; p.o.; once) does not damage the stomach and small intestine of helper arthritis rats^[1].
CJ-042794 (3-45 mg/kg; p.o.; twice daily for 14 d; Sprague-Dawley rats) promotes spontaneous healing of gastric ulcers^[1].
CJ-042794 (10 mg/kg; p.o.; daily, for 7 d) repeats administration impairs the healing of chronic gastric ulcers with a down-regulation of vascular endothelial growth factor expression in the ulcerated mucosa^[1].