产品说明书
Lixisenatide
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同义名 : | 利西拉肽 ;Lyxumia;Adlyxin;AVE0010;ZP10A peptide |
| CAS号 : | 320367-13-3 | |
| 货号 : | A1142139 | |
| 分子式 : | - | |
| 纯度 : | 99+% | |
| 分子量 : | 0 | |
| MDL号 : | MFCD13194768 | |
| 存储条件： |
粉末 Sealed in dry,Store in freezer, under -20°C 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
H2O: 100 mg/mL，配合低频超声助溶 |
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| 动物实验配方： |
| 生物活性 | |||
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| 描述 | Lixisenatide is a synthetic, potent and selective GLP-1 receptor agonist with Ki value of 1.33nM. It is used in the treatment for type 2 diabetes mellitus (T2DM) and suggests actions that are highly relevant to the long-term maintenance of glucose homeostasis. Lixisenatide is a 44 amino acid peptide and shares similar sequence with pharmacologically active forms of human GLP-1 or exendin-4. ZP10A demonstrated dose-dependent improvement of glucose tolerance with an ED50 value of 0.02 nmol/kg i.p. in an oral glucose tolerance test (OGTT) in diabetic db/db mice. Long-term stimulation by Lixisenatide at 10nM for 24h led increased level of Akt-phosphorylation in INS-1 cells. Lixisenatide at 10nM protected rat-derived β-cell line, Ins-1 cells, from both lipid- and cytokine-induced apoptosis. Also it prevented lipotoxicity-induced insulin depletion in human islets and preserved insulin production, storage and pancreatic β-cell function in vitro. Lixisenatide improved basal blood glucose and HbA1c with a rapid onset and sustained duration of action, and prevented the deterioration of pancreatic responsiveness and glucose homeostasis in animal models of diabetes. It delayed gastric emptying and reduced food intake. | ||
| 作用机制 | Lixisenatide is a GLP-1 analogue. | ||