Exendin-4 (Acetate)

Description

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 .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.

Uses

Exendin-4 acetate (Exenatide acetate), a 39 amino acid peptide, is a long-acting glucagon-like peptide-1 receptor agonist with an IC50 of 3.22 nM.

in vivo

References

1. Clardy, S.M., Mohan, J.F., Vinegoni, C., et al. Rapid, high efficiency isolation of pancreatic β-cells Sci. Rep. 5,13681(2015).
2. Doyle, M.E., Theodorakis, M.J., Holloway, H.W., et al. The importance of the nine-amino acid C-terminal sequence of exendin-4 for binding to the GLP-1 receptor and for biological activity Regul. Pept. 114(2-3),153-158(2003).
3. Nalin, L., Selvaraju, R.K., Velikyan, I., et al. Positron emission tomography imaging of the glucagon-like peptide-1 receptor in healthy and streptozotocin-induced diabetic pigs Eur. J. Nucl. Med. Mol. Imaging 41(9),1800-1810(2014).
4. Zhang, L., Zhang, L., Li, Y., et al. The novel dual GLP-1/GIP receptor agonist DA-CH5 is superior to single GLP-1 receptor agonists in the MPTP model of Parkinson’s disease J. Parkinsons Dis. 10(2),523-542(2020).