Exendin-4 (48-86) amide (acetate)

Exendin-4 (48-86) amide is a 39-amino acid peptide fragment corresponding to residues 48-86 of exendin-4, a peptide produced in the salivary gland of the Gila monster, and an agonist of the glucagon-like peptide 1 receptor (GLP-1R; IC50 = 3.5 nM).1,2 Radiolabeled exendin-4 (48-86) amide localizes to the pancreas, kidneys, and bladder in a porcine model of diabetes induced by streptozotocin (Item No. 13104).3 Exendin-4 (48-86) amide (10 nmol/kg) improves motor performance in the rotarod test in an mouse model of Parkinson’s disease induced by MPTP.4 It reduces MPTP-induced loss of dopaminergic neurons in the substantia nigra in the same model. Formulations containing exendin-4 (48-86) amide have been used in the treatment of type 2 diabetes mellitus.WARNING This product is not for human or veterinary use.

A GLP-1R agonist

4246.6

≥95%

Biochemicals/Peptides/Receptor Pharmacology/Agonists

Synonyms:Exenatide Acetate

NC([C@H](CO)NC([C@@H]1CCCN1C([C@@H]2CCCN2C([C@@H]3CCCN3C([C@@H](NC(CNC([C@H](CO)NC([C@H](CO)NC([C@@H

C184H282N50O60S • C2H4O2

914454-01-6

≥ 4 years

PBS (pH 7.2): 3 mg/ml

1.Eng, J.,Kleinman, W.A.,Singh, L., et al. Isolation and characterization of exendin-4, an exendin-3 analogue, from Heloderma suspectum venom. Further evidence for an exendin receptor on dispersed acini from guinea pig pancreas. The Journal of Biological Chemisty 267(11), 7402-7405 (1992).
2.Göke, R.,Fehmann, H.C.,Linn, T., et al. Exendin-4 is a high potency agonist and truncated exendin-(9-39)-amide an antagonist at the glucagon-like peptide 1-(7-36)-amide receptor of insulin-secreting β-cells. The Journal of Biological Chemisty 268(26), 19650-19655 (1993).
3.Thorens, B.,Porret, A.,Bühler, L., et al. Cloning and functional expression of the human islet GLP-1 receptor. Demonstration that exendin-4 is an agonist and exendin-(9-39) an antagonist of the receptor. Diabetes 42(11), 1678-1682 (1993).
4.Donnelly, D. The structure and function of the glucagon-like peptide-1 receptor and its ligands. British Journal of Pharmacology 166(1), 27-41 (2012).
5.Perry, T.,Haughey, N.J.,Mattson, M.P., et al. Protection and reversal of excitotoxic neuronal damage by glucagon-like peptide-1 and exendin-4. Journal of Pharmacology and Experimental Therapeutics 302(3), 881-888 (2002).
6.Komsuoglu Celikyurt, I.,Mutlu, O.,Ulak, G., et al. Exenatide treatment exerts anxiolytic- and antidepressant-like effects and reverses neuropathy in a mouse model of type-2 diabetes. Med.Sci.Monit.Basic Res. 20, 112-117 (2014).
7.van Bloemendaal, L.,Ten Kulve, J.S.,la Fleur, S.E., et al. Effects of glucagon-like peptide 1 on appetite and body weight: Focus on the CNS. Journal of Endocrinology 221(7), T1-T16 (2014).