Lixisenatide
Lixisenatide
CAS: 320367-13-3
Molecular Formula: C215H347N61O65S
Lixisenatide - Names and Identifiers
| Name | Lixisenatide |
| Synonyms | Lixisenatide lixisenatide Lixisenatide Acetate |
| CAS | 320367-13-3 |
Lixisenatide - Physico-chemical Properties
| Molecular Formula | C215H347N61O65S |
| Molar Mass | 4858.53 |
| Storage Condition | -20°C |
| In vitro study | Lixisenatide protects Ins-1 cells (a rat-derived beta cell line) from lipid-and cytokine-induced apoptosis. In human pancreatic islets, Lixisenatide also prevents lipotoxicity-induced insulin depletion (depletion) and maintains insulin production, storage, and pancreatic beta cell function. Binding experiments in CHO-K1 cells overexpressing human GLP-1 receptors have shown that Lixisenatide is a very potent and selective GLP-1 receptor agonist with binding affinity of Lixisenatide (Ki = 1.33±0.22 nM) it is more than 4 times the human GLP-1(Ki = 5.09±1.19 nM). In more than 80 different binding experiments, Lixisenatide did not interact with other potential drug targets, indicating its high selectivity for GLP-1 receptors. |
| In vivo study | The Half-Life of Lixisenatide is 2-4 hours, which is short compared to long-acting GLP-1-derived peptides such as liraglutide and albiglutide, so it is classified as a short-acting GLP-1 receptor agonist. Lixisenatide significantly improved glucose-responsive insulin secretion. In healthy normoglycemic dogs, a single subcutaneous injection of lixisenatide will cause a reduction in glucose concentration dependence after oral glucose screening and significantly reduce postprandial glucose excursions without increasing insulin concentrations. The effect of Lixisenatide on postprandial glucose excursions in dogs is, at least in part, associated with inhibition of gastric emptying and delayed intestinal glucose absorption. In the db/db mouse model and ZDF rat model, lixisenatide will also cause a concentration-dependent decrease in blood glucose after its oral glucose screening, an activity that is glucose-dependent, no effect on physiological glucose concentrations. In db/db mice, chronic lixisenatide administration prevented a sustained worsening of glucose tolerance, which was associated with a significant concentration-dependent decrease in glycosylated hemoglobin (HbA1c). In ZDF rats, subcutaneous infusion of 50 μg/kg/day lixisenatide for 12 weeks significantly reduced basal blood glucose and improved oral glucose tolerance. In rats with normal blood glucose, there is no hypoglycemic effect and no change in HbA1c levels. Lixisenatide can maintain the total amount and function of β cells by stimulating islet cell proliferation and regeneration and inhibiting islet cell apoptosis. Lixisenatide maintains pancreatic responsiveness in diabetic animals. |
Lixisenatide - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 0.206 ml | 1.029 ml | 2.058 ml |
| 5 mM | 0.041 ml | 0.206 ml | 0.412 ml |
| 10 mM | 0.021 ml | 0.103 ml | 0.206 ml |
| 5 mM | 0.004 ml | 0.021 ml | 0.041 ml |
Last Update：2024-01-02 23:10:35
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