Exendin-4 CAS 141758-74-9 Exenatide Acetate Salt Exenatide
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Characteristic:
Common name | Exenatide | English name | Exenatide acetate salt |
---|---|---|---|
CAS number | 141758-74-9 |
Molecular formula | C184H282N50O60S |
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Molecular weight | 4186.57000 |
Accurate mass | 4184.03000 |
PSA | 1775.05000 |
Storage conditions | Sealed, store at -20ºC |
Stability | No decomposition, no known hazardous reactions if used and stored according to specifications |
Usage:
Exenatide is the first drug in a new class of anti-diabetics known as the incretin mimetics, and it is indicated as adjunctive therapy to improve glycemic control in patients with type 2 diabetes who are taking metformin, a sulfonylurea, or both, but have not achieved adequate glycemic control. Exenatide is a functional analog of the human incretin Glucagon-Like Peptide-1 (GLP-1). GLP-1 is naturally released from cells in the GI tract in response to food intake and acts on its receptor on b-cells to potentiate glucose-stimulated insulin secretion. Exenatide is a long-acting agonist at the GLP-1 receptor. It is a synthetic version of a 39-amino acid peptide found in the salivary secretions of the Gila monster lizard.also moderates peak serum glucagon levels during hyperglycemic periods following meals, but does not interfere with glucagon release in response to hypoglycemia. The dosing regimen for exenatide is 5 or 10 mg twice daily, administered as a subcutaneous injection within an hour before morning and evening meals. Following subcutaneous administration, peak plasma concentrations of exenatide are reached in 2.1 h, and the plasma pharmacokinetic profile is dose proportional. The most common adverse events reported with exenatide include nausea, vomiting, diarrhea, feeling jittery, dizziness, headache, and dyspepsia.
Exendin-4 can activate the GLP-1 receptor, the receptor can increase cAMP levels of pancreatic acinar cells in intracellular , but it has no effect on VIP receptor.
Exendin-4 has been used as incretin mimetics for the treatment in HepG2 cells to exclude the influence of auxiliary material. It has also been used as an r (GLP-1R) agonist to exclude interference from auxiliary material.