| Identification | Back Directory | [Name]
Exendin-4 (Acetate) | [CAS]
914454-01-6 | [Synonyms]
Exendin-4 (Acetate)
Exenatide acetate
(Exendin-4 acetate)
Exendin-4 Acetate,Exenatide acetate, >98% | [Molecular Formula]
C186H285N50O62RS | [MOL File]
914454-01-6.mol | [Molecular Weight]
4245.62 |
| Hazard Information | Back Directory | [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]
Both low- and high-dose Exendin-4 treatment in ob/ob mice improve serum ALT and reduce serum glucose, and calculated HOMA scores compared with control. Exendin-4-treated ob/ob mice sustain a marked reduction in the net weight gain in the final 4 weeks of the study period[4]. Animals treated with Exendin-4 have more pancreatic acinar inflammation, more pyknotic nuclei and weigh significantly less than control rats. Exendin-4 treatment is associated with lower leptin levels as well as lower HOMA values in rats[5]. Exenatide causes dose-dependent relaxation of rat thoracic aorta, which is evoked via the GLP-1 receptor and is mediated mainly by H2S but also by NO and CO[6]. | [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). |
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