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Submit ReviewExendin-4
Description: Potent GLP-1 receptor agonist
Alternative Names: Exenatide,AC 2993
Purity: ≥95% (HPLC)
Biological Activity for Exendin-4
Exendin-4 is a high affinity glucagon-like peptide 1 (GLP-1) receptor agonist (Kd = 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 for Exendin-4
| M. Wt | 4186.61 |
| Formula | C184H282N50O60S |
| Sequence |
HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS (Modifications: Ser-39 = C-terminal amide) |
| Storage | Store at -20°C |
| Purity | ≥95% (HPLC) |
| CAS Number | 141758-74-9 |
| PubChem ID | 16157882 |
| InChI Key | HTQBXNHDCUEHJF-XWLPCZSASA-N |
| Smiles | [H]N[C@@H](CC1=CNC=N1)C(=O)NCC(=O)N[C@@H](CCC(O)=O)C(=O)NCC(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CC1=CC=CC=C1)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC1=CC=CC=C1)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC1=CNC2=C1C=CC=C2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)NCC(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(N)=O |
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.
Solubility Data for Exendin-4
| Solubility | Soluble to 1 mg/ml in water |
Product Datasheets for Exendin-4
References for Exendin-4
References are publications that support the biological activity of the product.
Eng et al (1992) Isolation and characterization of exendin-4, an exendin-3 analogue, from Heloderma suspectum venom. J.Biol.Chem. 267 7402 PMID: 1313797
Goke et al (1993) 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. J.Biol.Chem. 268 19650 PMID: 8396143
Thorens et al (1993) 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 1678 PMID: 8405712
Perry et al (2002) Protection and reversal of excitotoxic neuronal damage by glucagon-like peptide-1 and exendin-4. J.Pharmacol.Exp.Ther. 302 881 PMID: 12183643
Wang et al (2021) Exendin-4 improves long-term potentiation and neuronal dendritic growth in vivo and in vitro obesity condition. Sci.Rep. 11 8326 PMID: 33859286
If you know of a relevant reference for Exendin-4, please let us know.
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Keywords: Exendin-4, Exendin-4 supplier, Potent, GLP-1, receptor, agonists, Receptors, Glucagon-Like, Peptide, 1, AC2993, Ex4, exenatide, neuroprotective, neuroinflammation, neurotoxicity, LTP, Exenatide, AC, 2993, 1933, Tocris Bioscience
8 Citations for Exendin-4
Citations are publications that use Tocris products. Selected citations for Exendin-4 include:
Wang et al (2013) Glucagon-like peptide-1 protects against cardiac microvascular injury in diabetes via a cAMP/PKA/Rho-dependent mechanism. PLoS One 62 1697 PMID: 23364453
Suissa et al (2013) Gastrin: a distinct fate of neurogenin3 positive progenitor cells in the embryonic pancreas. ACS Chem Biol 8 e70397 PMID: 23940571
Vallof et al (2019) Glucagon-like peptide-1 receptors within the nucleus of the solitary tract regulate alcohol-mediated behaviors in rodents. Neuropharmacology 149 124 PMID: 30772374
Jazayeri (2017) Crystal structure of the GLP-1 receptor bound to a peptide agonist. Nature 546 254 PMID: 28562586
Lutter (2017) Novel and ultra-rare damaging variants in neuropeptide signaling are associated with disordered eating behaviors. PLoS One 12 e0181556 PMID: 28846695
Jesinkey et al (2019) Mitochondrial GTP Links Nutrient Sensing to β Cell Health, Mitochondrial Morphology, and Ins. Secretion Independent of OxPhos. Cell Rep 28 759 PMID: 31315053
Tuesta (2017) GLP-1 acts on habenular avoidance circuits to control nicotine intake. Nat Neurosci 20 708 PMID: 28368384
Pritchett and Hajnal (2012) Glucagon-like peptide-1 regulation of carbohydrate intake is differentially affected by obesogenic diets. Obesity (Silver Spring) 20 313 PMID: 22134200
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Literature in this Area
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