Glucagon-like peptide-1 receptor (GLP1R) GPCR Assay for compound screening and profiling in cells
GLP1R is the receptor for glucagon-like peptide-1 (GLP-1), an incretin hormone released postprandially from intestinal L-cells. Upon activation by GLP-1, GLP1R stimulates adenylate cyclase, increasing intracellular cAMP levels. This leads to enhanced glucose-dependent insulin secretion, suppressed glucagon release, delayed gastric emptying, and increased satiety. These effects contribute to glycemic control and weight regulation.
GLP1R
Glucagon-like peptide 1 receptor
HEK293
Transfected
HEK293 cells were transduced with a human Glucagon-like peptide 1 receptor (GLP1R). Stimulation of these cells with Liraglutide, an artificial long-acting GLP-1 analog, results in agonistic activation of cAMP-release, which can be measured by FRET technology, resulting in signal reduction upon cAMP-release. The assay has been validated based on flow detection of target expression on cells and response to known GLP1R agonists.
Induction of cAMP release
Freiburg, Germany
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Reference compound IC50 for GLP1R
Liraglutide is known to specifically activate the cAMP response as agonist of glucagon-like peptide-1 receptor (GLP-1R). Measured by FRET technology, increased cAMP levels result in signal reduction. The agonist was included for the validation process and the cellular GLP1-R assay generated highly reproducible IC50 values. The graph shows a representative result. A cAMP-standard dose response curve was generated in parallel.