| 产品描述： | 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 |
| 靶点： |
EP:10 nM (EC50) |
| 体内研究： |
CJ-042794 (CJ-042794; 0.3-3 mg/kg; i.d.; once) antagonizes the HCO3 stimulatory action of AE1-329 in the duodenum. 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. CJ-042794 (30 and 50 mg/kg; p.o.; once) does not damage the stomach and small intestine of helper arthritis rats. CJ-042794 (3-45 mg/kg; p.o.; twice daily for 14 d; Sprague-Dawley rats) promotes spontaneous healing of gastric ulcers. 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. Animal Model: Male Sprague-Dawley rats (200-230 g) Dosage: 0.3, 1, and 3 mg/kg Administration: intradermal injection; once Result: Attenuated the PGE2-stimulated HCO3 secretion in a dose-dependent manner and had the inhibition being 68.9% at 1 mg/kg. |
| 参考文献： |
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. |
| 溶解性： |
Soluble in DMSO |
| 保存条件： |
-80℃（运输条件：冰袋低温运输） |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.416 ml |
12.082 ml |
24.165 ml |
| 5 mM |
0.483 ml |
2.416 ml |
4.833 ml |
| 10 mM |
0.242 ml |
1.208 ml |
2.416 ml |
| 50 mM |
0.048 ml |
0.242 ml |
0.483 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京