BETP --- GLP-1R Potentiator
Overview | |
Catalog # | bs-60196c-2-mg-solid |
Product Name | BETP --- GLP-1R Potentiator |
Specifications | |
Storage Buffer | Powder |
Storage Condition | Store in dry, dark place at -20C for 1 year. |
Target | |
Product Information | Molecular Weight: 406.42 Formula: C20 H17 F3 N2 O2 S CAS Number: 1371569-69-5 InChi Key: NTDFYGSSDDMNHI-UHFFFAOYSA-N InChi: InChI=1S/C20H17F3N2O2S/c1-2-28(26)19-24-17(12-18(25-19)20(21,22)23)15-9-6-10-16(11-15)27-13-14-7-4-3-5-8-14/h3-12H,2,13H2,1H3 Smiles: CCS(=O)C1N=C(C=C(N=1)C(F)(F)F)C1=CC(=CC=C1)OCC1C=CC=CC=1 Purity: 98.0 Solubility: DMSO up to 100 mM Appearance: Solid Power. Shelf Life: 1.0 years |
Description | BETP is positive allosteric modulator and partial agonist of the glucagon-like peptide 1 (GLP-1) receptor. It covalently modifies cysteines 347 and 438 in GLP-1R. Specificity studies have shown that it has no activity on GLP-2, GIP, PTH or glucagon receptors. BETP has been shown to potentiate GLP-1R–dependent intracellular calcium mobilization but not cAMP accumulation in response to GLP-1(7-36)NH2 in recombinant cell lines. Conversely, BETP can enhance cAMP efficacy of GLP-1(9-36)NH2 at GLP-1R but not intracellular calcium mobilization. BETP also potentiates cAMP production of the dual-acting GLP-1R/glucagon (GCG) receptor (GCGR) agonist oxyntomodulin at GLP-1R. It promotes GLP-1(9-36)NH2–mediated glucose-dependent insulin secretion in rodent and human islet preparations as well as in rodent models following intravenous administration. |