17-phenyl trinor Prostaglandin E2 ethyl amide (Synonyms:17-Phenyl trinor PGE2 ethyl amide)
目录号 : KCM10702 CAS No. : 1219032-20-8 纯度 : ≥98%
17-phenyl trinor PGE ethyl amide is derived from 17-phenyl trinor PGE, a synthetic analog of PGE that acts as an agonist of EP and EP receptors in mice (K = 14 and 3.7 nM, respectively) and EP, EP, and EP in rats (K = 25, 4.3, and 54 nM, respectively). 17-phenyl trinor PGE causes contraction of guinea pig ileum at a concentration of 11 µM and is 4.4 times more potent than PGE as an antifertility agent in hamsters. Modification of the C-1 carboxyl group to an ethyl amide serves to increase lipid solubility, thereby improving uptake into tissues and further lowering the effective concentration. Ethyl amide groups are then removed by amidases, regenerating the active free acid.
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生物活性

17-Phenyl trinor prostaglandin E2 ethyl amide (17-Phenyl trinor PGE2 ethyl amide) is a EP1 receptor agonist. 17-Phenyl trinor prostaglandin E2 ethyl amide aggravates renal dysfunction and glomerulosclerosis.

体内研究

17-Phenyl trinor prostaglandin E2 ethyl amide (0.3 µg/g; i.p.; three times a week for 12 weeks) aggravates renal dysfunction and glomerulosclerosis in five-sixths nephrectomy renal fibrosis model mice.

 

Animal Model: 8-12 weeks, 15-20 g, C57/BL6 male mice (five-sixths nephrectomy renal fibrosis model)
Dosage: 0.3 µg/g
Administration: I.p.; three times a week for 12 weeks
Result: Increased the plasma blood urea nitrogen (BUN) levels and plasma creatinine (Cr) concentration, increased the extracellular matrix and the area of collagen deposition, upregulated the protein of expression of Col1, GRP78, TRPC1 and PERK in 5/6 Nx mice.
分子式
C25H35NO4
分子量
413.6
CAS号
1219032-20-8
储存方式
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
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