Biological Activity
Selective positive allosteric modulator and partial agonist of the glucagon-like peptide 1 (GLP-1) receptor. Increases binding affinity of oxyntomodulin for the GLP-1 receptor. Potentiates oxyntomodulin-mediated GLP-1 receptor signaling in vitro and insulin secretion in vivo. Has no effect on GLP-2, GIP, PTH or glucagon receptors.
Compound Libraries
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Technical Data
| M. Wt | 406.42 |
| Formula | C20H17F3N2O2S |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1371569-69-5 |
| PubChem ID | 49868481 |
| InChI Key | NTDFYGSSDDMNHI-UHFFFAOYSA-N |
| Smiles | CCS(C1=NC(C2=CC=CC(OCC3=CC=CC=C3)=C2)=CC(C(F)(F)F)=N1)=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
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 40.64 | 100 | |
| ethanol | 20.32 | 50 |
Preparing Stock Solutions
The following data is based on the product molecular weight 406.42. 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 | 2.46 mL | 12.3 mL | 24.61 mL |
| 5 mM | 0.49 mL | 2.46 mL | 4.92 mL |
| 10 mM | 0.25 mL | 1.23 mL | 2.46 mL |
| 50 mM | 0.05 mL | 0.25 mL | 0.49 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Willard et al (2012) Small molecule allosteric modulation of the glucagon-like Peptide-1 receptor enhances the insulinotropic effect of oxyntomodulin. Mol.Pharmacol. 82 1066 PMID: 22930710
Sloop et al (2010) Novel small molecule glucagon-like peptide-1 receptor agonist stimulates insulin secretion in rodents and from human islets. Diabetes 59 3099 PMID: 20823098
Cheong et al (2012) Two small molecule agonists of glucagon-like peptide-1 receptor modulate the receptor activation response differently. Biochem.Biophys.Res.Comm. 417 558 PMID: 22177947
Keywords: BETP, supplier, Allosteric, modulators, GLP-1, GLP1, receptors, glucagon-like, peptide, agonists, Glucagon-Like, Peptide, 1, Receptors, Glucagon-Like, Peptide, 1, Receptors, Tocris Bioscience
