产品
编 号：F477501
分子式：C22H17ClFNO4
分子量：413.83
分子式：C22H17ClFNO4
分子量：413.83
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
5mg
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10mg
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50mg
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100mg
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结构图
CAS No: 847728-01-2
产品详情
生物活性：
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.
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 secretionin a dose-dependent manner and had the inhibition being 68.9% at 1 mg/kg.
Animal Model:Male Sprague-Dawley rats (200-230 g)
Dosage:30 and 50 mg/kg
Administration:Oral administration; once
Result:Did not produce any damage in the gastrointestinal mucosa.Did not produce gastric ulcerogenic response induced by cold-restraint stress.
Animal Model:Dark Agouti (DA) rats (140-160 g)
Dosage:30 and 50 mg/kg
Administration:Oral administration; once
Result:Caused any visible damage in the gastric mucosa of normal rats.Had little injurious effect on the small intestine of arthritic rats.
Animal Model:Male Sprague-Dawley rats (200-230 g)
Dosage:3, 10, and 45 mg/kg
Administration:Oral administration; twice daily for 14 days
Result:Healed ulcers gradually within 14 days, and the ulcer score on day 17 was 1.6 mm2.
Animal Model:Male Sprague-Dawley rats (200-230 g)
Dosage:10 mg/kg
Administration:Oral administration; daily for 7 days
Result:Down-regulates the expression of VEGF and decreased the angiogenic response.
体外研究：
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.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.
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.
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 secretionin a dose-dependent manner and had the inhibition being 68.9% at 1 mg/kg.
Animal Model:Male Sprague-Dawley rats (200-230 g)
Dosage:30 and 50 mg/kg
Administration:Oral administration; once
Result:Did not produce any damage in the gastrointestinal mucosa.Did not produce gastric ulcerogenic response induced by cold-restraint stress.
Animal Model:Dark Agouti (DA) rats (140-160 g)
Dosage:30 and 50 mg/kg
Administration:Oral administration; once
Result:Caused any visible damage in the gastric mucosa of normal rats.Had little injurious effect on the small intestine of arthritic rats.
Animal Model:Male Sprague-Dawley rats (200-230 g)
Dosage:3, 10, and 45 mg/kg
Administration:Oral administration; twice daily for 14 days
Result:Healed ulcers gradually within 14 days, and the ulcer score on day 17 was 1.6 mm2.
Animal Model:Male Sprague-Dawley rats (200-230 g)
Dosage:10 mg/kg
Administration:Oral administration; daily for 7 days
Result:Down-regulates the expression of VEGF and decreased the angiogenic response.
体外研究：
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.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.
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