Biological Activity
Potent and selective GLP-1 receptor antagonist (Kd = 1.7 nM at cloned human GLP-1 receptors). Inhibits cAMP production and insulin release induced by GLP-1 (7-36), exendin-3 (IC50 = 20 nM) and exendin-4. Blocks the inhibitory effect of GLP-1 on food intake in rats.
Technical Data
| M. Wt | 3369.79 |
| Formula | C149H234N40O47S |
| Sequence |
DLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS (Modifications: Ser-31 = C-terminal amide) |
| Storage | Desiccate at -20°C |
| CAS Number | 133514-43-9 |
| PubChem ID | 16198321 |
| InChI Key | WSEVKKHALHSUMB-MVNVRWBSSA-N |
| Smiles | [H]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 3369.79. 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 | 0.3 mL | 1.48 mL | 2.97 mL |
| 5 mM | 0.06 mL | 0.3 mL | 0.59 mL |
| 10 mM | 0.03 mL | 0.15 mL | 0.3 mL |
| 50 mM | 0.01 mL | 0.03 mL | 0.06 mL |
Molarity Calculator
Reconstitution Calculator
Dilution Calculator
Product Datasheets
References
References are publications that support the products' biological activity.
Raufman et al (1991) Exendin-3, a novel peptide from the Heloderma horridum venom, interacts with vasoactive intestinal peptide receptors and a newly described receptor on dispersed acini from guinea pig pancreas. J.Biol.Chem. 266 2897 PMID: 1704369
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
Turton et al (1996) A role for glucagon-like peptide-1 in the central regulation of feeding. Nature 379 69 PMID: 8538742
Keywords: Exendin-3 (9-39) amide, supplier, Potent, GLP-1, receptor, antagonists, Receptors, Glucagon-Like, Peptide, 1, Glucagon-Like, Peptide, 1, Receptors, Glucagon-Like, Peptide, 1, Receptors, Tocris Bioscience
