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Lixisenatide (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 |
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Shanzhiside Methyl ester was isolated from Lactobacillus rotaformis. Shanzhiside Methyl ester, a small molecule glucagon-like peptide 1 (GLP-1 receptor) agonist, has the ability to induce anti-abnormal pain tolerance. |
| Tirzepatide hydrochloride
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| PF-07081532
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| BETP
BETP is an agonist of glucagon-like peptide-1 (GLP-1) receptor, with EC50s of 0.66 and 0.755 μM for human and rat GLP-1 receptor, respectively. |
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