Biological Activity
High affinity glucagon-like peptide 1 (GLP-1) receptor agonist (Kd = 136 pM); originally isolated from Heloderma suspectum venom. Potently induces cAMP formation without stimulating amylase release in pancreatic acini. Potentiates glucose-induced insulin secretion in isolated rat islets. Protects against glutamate-induced neurotoxicity.
Technical Data
| M. Wt | 4186.61 |
| Formula | C184H282N50O60S |
| Sequence |
HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS (Modifications: Ser-39 = C-terminal amide) |
| Storage | Desiccate at -20°C |
| 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.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solubility | Soluble to 1 mg/ml in water |
Preparing Stock Solutions
The following data is based on the product molecular weight 4186.61. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 0.24 mL | 1.19 mL | 2.39 mL |
| 5 mM | 0.05 mL | 0.24 mL | 0.48 mL |
| 10 mM | 0.02 mL | 0.12 mL | 0.24 mL |
| 50 mM | 0 mL | 0.02 mL | 0.05 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
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 insulin-secreting 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
Keywords: Exendin-4, supplier, Potent, GLP-1, receptor, agonists, Receptors, Glucagon-Like, Peptide, 1, AC2993, Exenatide, AC, 2993, Glucagon-Like, Peptide, 1, Receptors, Glucagon-Like, Peptide, 1, Receptors, Tocris Bioscience
