| Description | CJ-42794 (CJ-042794) is a selective antagonist of prostaglandin E receptor subtype 4 (EP4). It inhibits [3H]-PGE2 binding to the human EP4 receptor (a mean pKi: 8.5). CJ-42794 is 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) (IC50 : 8.5 (pKi )). |
| In vitro | CJ-042794 competitively inhibits PGE2-evoked elevations of intracellular cAMP levels in HEK293 cells overexpressing human EP4receptor (mean pA2: 8.6). CJ-042794 reverses the inhibitory effects of PGE2 on LPS-induced TNFα production in a concentration-dependent manner [1]. |
| In vivo | CJ-42794 significantly delays ulcer healing in rats and mice and these responses were both attenuated by coadministration of CJ-42794 [2]. |
| Synonyms | CJ-042794 |
| molecular weight | 413.83 |
| Molecular formula | C22H17ClFNO4 |
| CAS | 847728-01-2 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | DMSO: 28 mg/mL (67.66 mM) |
| References | 1. Murase A, et al. In vitro pharmacological characterization of CJ-042794, a novel, potent, and selective prostaglandin EP(4) receptor antagonist. Life Sci. 2008 Jan 16;82(3-4):226-232. 2. Hatazawa R, et al. Cyclooxygenase-2/prostaglandin E2 accelerates the healing of gastric ulcers via EP4 receptors. Am J Physiol Gastrointest Liver Physiol. 2007 Oct;293(4):G788-97. |