Key Features:
High Sensitivity: The cell line offers high signal-to-background with over 500-fold induction, ensuring accurate and reproducible results in CREB pathway studies.
Sensitive and Quantitative: The luciferase reporter provides a direct and reliable readout of CREB activation, enabling precise measurement of pathway activity.
Mutation-Specific Applications: Co-expression of the A416T GLP-1R variant and a CREB-responsive luciferase reporter enables characterization of how this clinically relevant mutation alters GLP-1R signaling cascades. Suitable for functional studies, ligand screening, and dose-response profiling of compounds in the context of the A416T variant.
Stable Integration: Established via co-transfection with GLP1R and CRE-luciferase constructs, followed by antibiotic selection and functional screening withDanuglipron and Exendin-4.
 
The GLP-1R(A416T)/CREB Luciferase Reporter HEK293 Stable Cell Line is derived from human embryonic kidney cells and stably expresses glucagon-like peptide-1 receptor (GLP-1R) carrying the A416T point mutation alongside a firefly luciferase reporter gene under the control of the cAMP response element-binding protein (CREB) response element. This dual-expression cell line is an ideal tool for monitoring intracellular signaling dynamics specifically arising from the A416T receptor variant.

GLP-1R is a G protein-coupled receptor (GPCR) that normally signals via cAMP/PKA and activates CREB. The A416T substitution, located in the receptor’s transmembrane region, may alter ligand binding, receptor conformational changes, or downstream signaling strength. Activation of CREB leads to luciferase expression, providing a convenient and quantitative readout of signaling differences compared to wild-type GLP1R.

This cell line is ideal for studying the functional impact of the GLP1R A416T variant on signaling, screening for GPCR modulators, and investigating cAMP/PKA/CREB pathway dynamics. It is particularly useful for drug discovery programs targeting metabolic diseases, including type 2 diabetes and obesity.
 
This versatile cell line serves as a powerful in vitro tool for both basic research and translational applications in endocrinology, pharmacology, and metabolic disease research.