Lixisenatide (Lyxumia, Adlyxin, ZP10A peptide) is a glucagon-like peptide-1 (GLP-1) receptor agonist, which is a hormone that helps normalize blood sugar levels. Lixisenatide protects Ins-1 cells (a rat-derived β-cell line) from both lipid- and cytokine-induced apoptosis. Lixisenatide also prevents lipotoxicity-induced insulin depletion in human islets and preserves insulin production, storage and pancreatic β-cell function in vitro.
In ZDF rats, a continuous subcutaneous infusion of lixisenatide 50 μg/kg/day for 12 weeks significantly decreases basal blood glucose and improves oral glucose tolerance compared with control animals. It has no hypoglycemic effect and does not change HbA1c in normoglycemic rats. Lixisenatide can maintain beta cell mass and function through stimulation of islet cell proliferation and neogenesis, and inhibition of islet cell apoptosis.
| Cell Experiment | |
|---|---|
| Cell lines | both cytokine- and FFA-treated cells |
| Preparation method | In both cytokine- and FFA-treated cells, Lixisenatide (10 nM) significantly decreased caspase-3 activity, and decreased the amount of apoptotic cells by 50–60% (similar to the effect seen with 10 nM GLP-1 or exendin-4) . |
| Concentrations | 10 nM |
| Incubation time | - |
| Animal Experiment | |
|---|---|
| Animal models | |
| Formulation | |
| Dosages | |
| Administration | |
| Molecular Weight | 4858.53 |
| Formula | C215H347N61O65S |
| CAS Number | 320367-13-3 |
| Solubility (25°C) | Water 90 mg/mL |
| Storage | -20°C, dry, sealed |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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