Eicosapentaenoic acid ethyl ester

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Chemical Structure| 86227-47-6 同义名 : 顺-二十碳五烯酸乙酯 ;EPA ethyl ester; Ethyl eicosapentaenoate; Icosapent ethyl; AMR101
CAS号 : 86227-47-6
货号 : A759947
分子式 : C22H34O2
纯度 : 98% contains 2000ppm alpha-tocopherol as stabilizer
分子量 : 330.5
MDL号 : MFCD00673476
存储条件:

Pure form Keep in dark place, inert atmosphere, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 105 mg/mL(317.7 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

无水乙醇: 50 mg/mL(151.28 mM),配合低频超声助溶,注意:无水乙醇开封后,易挥发,也会吸收空气中的水分,导致溶解能力下降,请避免使用开封较久的乙醇

生物活性
描述 Eicosapentaenoic acid ethyl ester is an omega-3 fatty acid agent. The enhanced contractile response by phenylephrine in diabetic mice was not altered by the administration of EPA-E (10 mg/day). In addition, the direct administration of EPA-E metabolites such as EPA, docosahexaenoic acid, and docosapentaenoic acid led to vasodilation in the aortic rings of C57BL/6 J mice. Chronic EPA-E administration prevented the development of endothelial dysfunction in KKAy mice, partly via the direct action of EPA-E metabolites on the aorta[3]. Oral administration of EPA-E ameliorated skin barrier dysfunction and pruritus in AD mice. In the SC of AD mice, covalently bound Cer were markedly diminished[4].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01002118 Cardiovascular Disease Not Applicable Terminated(Unable to recruit e... 展开 >>ligible subjects; no data analyzed) 收起 << - United States, Iowa ... 展开 >> University of Iowa Iowa City, Iowa, United States, 52242 收起 <<
NCT00504309 Hypertriglyceridemia Not Applicable Completed - United States, Pennsylvania ... 展开 >> Penn State University General Clinical Research Center University Park, Pennsylvania, United States, 16802 收起 <<
NCT01056133 Non-alcoholic Fatty Liver Dise... 展开 >>ase Non-alcoholic Steatohepatitis 收起 << Phase 2 Completed - Canada, Ontario ... 展开 >> University Health Network, Toronto General Hospital Toronto, Ontario, Canada, M5G 1Z5 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.03mL

0.61mL

0.30mL

15.13mL

3.03mL

1.51mL

30.26mL

6.05mL

3.03mL

参考文献

[1]Jacobson TA. A new pure ω-3 eicosapentaenoic acid ethyl ester (AMR101) for the management of hypertriglyceridemia: the MARINE trial. Expert Rev Cardiovasc Ther. 2012 Jun;10(6):687-95.

[2]Bays HE, Ballantyne CM, et al. Eicosapentaenoic acid ethyl ester (AMR101) therapy in patients with very high triglyceride levels (from the Multi-center, plAcebo-controlled, Randomized, double-blINd, 12-week study with an open-label Extension [MARINE] trial). Am J Cardiol. 2011 Sep 1;108(5):682-90.

[3]Takenouchi Y, Ohtake K, Nobe K, Kasono K. Eicosapentaenoic acid ethyl ester improves endothelial dysfunction in type 2 diabetic mice. Lipids Health Dis. 2018 May 22;17(1):118

[4]Fujii M, Ohyanagi C, Kawaguchi N, Matsuda H, Miyamoto Y, Ohya S, Nabe T. Eicosapentaenoic acid ethyl ester ameliorates atopic dermatitis-like symptoms in special diet-fed hairless mice, partly by restoring covalently bound ceramides in the stratum corneum. Exp Dermatol. 2018 Aug;27(8):837-840