Calcium Flux Assay

HTS163L - ChemiBrite™ GLP-1 Glucagon Family Receptor Stable Cell Line

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    Glucagon-like peptide-I (GLP-1), a member of the glucagon-secretin peptide family, is secreted from L-cells of the small intestine and binds to a class B (class 2) G protein-coupled receptor (Mayo et al. 2003). The GLP-1 receptor is expressed in pancreatic beta cells and upon binding to GLP-1, it couples to Gs to increase cAMP levels and insulin secretion (Drucker et al. 1987). In addition, GLP-1 has been shown to delay gastric emptying and regulate appetite. Therefore, the GLP-1 receptor represents an important therapeutic target for type II diabetes. In addition, the degradation-resistant analog of GLP-1, exanatide, is used clinically in combination with other glucose-lowering drugs to control type II diabetes (D’Alessio et al. 2004). Eurofins' cloned human GLP-1 receptor-expressing ChemiBrite cells were made by stable transfection of HEK293 cells with ChemiBrite clytin and the GLP-1 receptor and a promiscuous G protein to couple the receptor to the calcium signaling pathway. These stability-tested cells are ready for luminescent analysis of agonists, antagonists and modulators at the GLP-1 receptor.

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    Item Unit of Measure: PK
    Contents: 2 vials of mycoplasma-free cells, 1 ml per vial.
    Storage: Vials are to be stored in liquid N2.
    Applications: Calcium Flux Assay, cAMP Accumulation
    Entrez Gene Number: NM_0002062
    Host Cell: HEK293
    Exogenous Gene Expression: Human GLP-1 cDNA (Accession Number: NM_002062; see CODING SEQUENCE below) and a proprietary mutant clytin photoprotein and promiscuous G protein expressed in a bicistronic vector
    GMO: This product contains genetically modified organisms.
    Reference 1: 1. Mayo KE et al. (2003) International Union of Pharmacology. XXXV. The glucagon receptor family. Pharmacol. Rev. 55: 167-194.
    Reference 2: 2. Drucker et al. (1987) Glucagon-like peptide I stimulates insulin gene expression and increases cyclic AMP levels in rat islet cell line. Proc. Natl. Acad. Sci., 84: 3434-3438.
    Reference 3: 3. D’Alessio D et al. (2004) Glucagon-like peptide 1: evolution of an incretin into a treatment for diabetes. Am. J. Physiol. Endocrinol. Metab. 286: 882-890.
    Reference 4: 4. Thorens B 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: 1678-82.