名称
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Exendin-4
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别名
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Exendin4exenatide; Byetta
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序列(单字母缩写)
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HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS-NH2
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序列(三字母缩写)
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{HIS}{GLY}{GLU}{GLY}{THR}{PHE}{THR}{SER}{ASP}{LEU}{SER}{LYS}{GLN}{MET}{GLU}{GLU}{GLU}{ALA}{VAL}{ARG}{LEU}{PHE}{ILE}{GLU}{TRP}{LEU}{LYS}{ASN}{GLY}{GLY}{PRO}{SER}{SER}{GLY}{ALA}{PRO}{PRO}{PRO}{SER}-NH2
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C-端
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NH2
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基本描述
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Exendin-4 is a 39-amino acid peptide amide. Exendin-4, like Exendin-3, stimulates an increase in acinar cAMP without stimulating the release of amylase. Exendin-4 is a long-acting potent agonist of the glucagon-like peptide 1 (GLP-1). Exendin-4 is the active component of Byetta (exenatide) injection, which may improve glycemic control in people with type 2 diabetes mellitus and has the potential to reduce plasma glucose at least partly by a delay in gastric emptying as well as by reducing calorie intake. Exendin-4 enhances glucose-dependent insulin secretion by the pancreatic β-cell and suppresses inappropriately elevated glucagon secretion.
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溶解度
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Soluble in water. The contents of this vial have been accurately determined. Both the stopper and the vial have been siliconized. Do not attempt to weigh out a smaller portion of the contents.
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分子量
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4186.660
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化学式
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C184H282N50O60S
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纯度
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> 95%
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存储条件
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Store the peptide at -20°C.
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注释
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This peptide interacts interacts with exendin receptor to increase pancreatic acinar cAMP. It has no secretagogue activity and does not bind to VIP receptors.
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Documents
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Figures
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Reference
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Gardiner SM, et al. Mesenteric vasoconstriction and hindquarters vasodilatation accompany the pressor actions of exendin-4 in conscious rats. J. Pharmacol. Exp. Ther. Feb 2006; 316(2): 852-859.
Park S, et al. Exendin-4 uses Irs2 signaling to mediate pancreatic beta cell growth and function. J. Biol. Chem. Jan 2006; 281(2): 1159-1168.
Kim MJ, et al. Exendin-4 induction of cyclin D1 expression in INS-1 beta-cells: involvement of cAMP-responsive element. J. Endocrinol. Mar 2006; 188(3): 623-633.
Jain R., etc. Pharmacological inhibition of Eph receptors enhances glucose-stimulated insulin secretion from mouse and human pancreatic islets. Diabetologia. 2013 Jun;56(6):1350-1355.
Shiraishi D., etc. Glucagon-Like Peptide-1 (Glp-1) Induces M2 Polarization Of Human Macrophages Via Stat3 Activation. Biochem Biophys Res Commun. 2012 Aug;425(2):304 - 8.
Wei Gao and William J. Jusko.., etc. Pharmacokinetic and Pharmacodynamic Modeling of Exendin-4 in Type 2 Diabetic Goto-Kakizaki Rats. J Pharmacol Exp Ther. 2011 Mar;336(3):881 - 890.
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