Exendin-4

Biological Activity

Exendin-4 is a high affinity glucagon-like peptide 1 (GLP-1) receptor agonist (K_d = 136 pM); originally isolated from Heloderma suspectum venom. Exendin-4 potently induces cAMP formation without stimulating amylase release in pancreatic acini. Potentiates glucose-induced insulin secretion in isolated rat islets. Exendin-4 protects against glutamate-induced neurotoxicity, and in a mouse model of metabolic imblance it reduces neuroinflammation and enhances long-term-potentiation.

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

1. A programmable synthetic lineage-control network that differentiates human IPSCs into glucose-sensitive insulin-secreting beta-like cells
   P Saxena, BC Heng, P Bai, M Folcher, H Zulewski, M Fussenegge
   Nat Commun, 2016;7(0):11247.
2. The Hypothalamic Glucagon-Like Peptide-1 (GLP-1) Receptor (GLP-1R) is Sufficient but Not Necessary for the Regulation of Energy Balance and Glucose Homeostasis in Mice
   Melissa A Burmeister
   Diabetes, 2016;0(0):.
3. Expansion and conversion of human pancreatic ductal cells into insulin-secreting endocrine cells.
   Lee J, Sugiyama T, Liu Y, Wang J, Gu X, Lei J, Markmann J, Miyazaki S, Miyazaki J, Szot G, Bottino R, Kim S
   Elife, 2013;2(0):e00940.
4. Defined three-dimensional culture conditions mediate efficient induction of definitive endoderm lineage from human umbilical cord Wharton's jelly mesenchymal stem cells
   
   Stem Cell Res Ther, 2016;7(1):165.
5. Hindbrain oxytocin receptors contribute to the effects of circulating oxytocin on food intake in male rats.
   Ho J, Anekonda V, Thompson B, Zhu M, Curry R, Hwang B, Morton G, Schwartz M, Baskin D, Appleyard S, Blevins J
   Endocrinology, 2014;155(8):2845-57.
6. Protection and reversal of excitotoxic neuronal damage by glucagon-like peptide-1 and exendin-4.
   Perry et al.
   J.Pharmacol.Exp.Ther., 2002;302:881
7. 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 Ins-Secr.g β-cells.
   Goke et al.
   J.Biol.Chem., 1993;268:19650
8. 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.
   Thorens et al.
   Diabetes, 1993;42:1678
9. Isolation and characterization of exendin-4, an exendin-3 analogue, from Heloderma suspectum venom.
   Eng et al.
   J.Biol.Chem., 1992;267:7402

Product Datasheets