| Bioactivity | 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]. | ||||||||||||
| Invitro | 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]. Animal Model: | ||||||||||||
| Name | CJ-42794 | ||||||||||||
| CAS | 847728-01-2 | ||||||||||||
| Formula | C22H17ClFNO4 | ||||||||||||
| Molar Mass | 413.83 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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):226-32. [2]. Takeuchi K, et, al. Effect of (S)-4-(1-(5-chloro-2-(4-fluorophenyoxy)benzamido)ethyl) benzoic acid (CJ-42794), a selective antagonist of prostaglandin E receptor subtype 4, on ulcerogenic and healing responses in rat gastrointestinal mucosa. J Pharmacol Exp Ther. 2007 Sep;322(3):903-12. |
CJ-42794
CAS: 847728-01-2 F: C22H17ClFNO4 W: 413.83
CJ-42794 (CJ-042794) is a potent, orally active, selective prostaglandin E receptor 4 (EP4) antagonist with an IC50 valu
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