CAS: 133514-43-9; Exendin (9-39)

该化合物是一种该化合物是一种类似 glucagon Peptide-1 (GLP-1) 的受体者. 它来自 exendin-4 , 一种在 Gila 怪物毒液中发现的自然产生的peptide . 它具有竞争性地抑制 GLP-1 受体活化, 使它成为研究 GLP-1 中介生理过程(如葡萄糖代谢和胰岛分泌)的宝贵工具. 它的氨化改变会增强稳定性和生物利用率, 提高其在研究应用中的效用. Exendin (9-39) amide 被广泛用于临床前研究, 调查 GLP-1 在胃调节, 胰腺功能和代谢紊乱的潜在治疗干预措施中的作用 .

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    专利信息


    专利号:US-7888116-B2
    优先权日:2004-07-22
    标 题 :Uses of notch receptors, notch ligands, and notch modulators in methods related to metabolic diseases
    发明人:EGAN JOSEPHINE M; DOYLE MAIRE E
    权利人:US HEALTH
    摘要:Disclosed are methods for identifying and isolating a precursor cell. Also, disclosed are methods of increasing insulin synthesis from a pancreatic B-cell. Further, disclosed are methods of improving pancreatic B-cell function. Still further, disclosed are methods of preventing or delaying the onset of a metabolic disease, methods of treating or preventing a metabolic disease in a subject, and to compositions for treating or preventing a metabolic disease in a subject in need of such treatment or prevention.

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    主要参考文献


    1: Tan M, Lamendola C, Luong R, McLaughlin T, Craig C. Safety, efficacy and pharmacokinetics of repeat subcutaneous dosing of avexitide (exendin 9-39) for treatment of post-bariatric hypoglycaemia. Diabetes Obes Metab. 2020 Aug;22(8):1406-1416. doi: 10.1111/dom.14048. Epub 2020 May 4.
    2: Craig CM, Lawler HM, Lee CJE, Tan M, Davis DB, Tong J, Glodowski M, Rogowitz E, Karaman R, McLaughlin TL, Porter L. PREVENT: A Randomized, Placebo-Controlled Crossover Trial of Avexitide for Treatment of Post-Bariatric Hypoglycemia. J Clin Endocrinol Metab. 2021 Feb
    22:dgab103. doi: 10.1210/clinem/dgab103. Epub ahead of print.

    合成参考文献


    参考文献:10.1111/j.1365-2982.2010.01476.x
    摘要:Amato A, Cinci L, Rotondo A, Serio R, Faussone-Pellegrini MS, Vannucchi MG, Mulè F. Peripheral motor action of glucagon-like peptide-1 through enteric neuronal receptors. Neurogastroenterol Motil. 2010 Jun;22(6):664–e203. doi: 10.1111/j.1365-2982.2010.01476.x.
    参考文献:10.1007/s00210-011-0665-3
    摘要:Ku HC, Chen WP, Su MJ. DPP4 deficiency preserves cardiac function via GLP-1 signaling in rats subjected to myocardial ischemia/reperfusion. Naunyn Schmiedebergs Arch Pharmacol. 2011 Aug;384(2):197–207. doi: 10.1007/s00210-011-0665-3.
    参考文献:10.1016/j.ejphar.2011.06.036
    摘要:Chan SW, Lin G, Yew DT, Rudd JA. A physiological role of glucagon-like peptide-1 receptors in the central nervous system of Suncus murinus (house musk shrew). Eur J Pharmacol. 2011 Oct 01;668(1-2):340–6. doi: 10.1016/j.ejphar.2011.06.036.
    参考文献:10.1172/jci25764
    摘要:Knauf C, Cani PD, Perrin C, Iglesias MA, Maury JF, Bernard E, Benhamed F, Grémeaux T, Drucker DJ, Kahn CR, Girard J, Tanti JF, Delzenne NM, Postic C, Burcelin R. Brain glucagon-like peptide-1 increases insulin secretion and muscle insulin resistance to favor hepatic glycogen storage. J Clin Invest. 2005 Dec;115(12):3554–63.
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