G protein-coupled receptor (GPCR)
Luciferase Reporter Cell Lines
Obesity and diabetes are major global health challenges linked to cardiovascular disease, type 2 diabetes, MASH, and certain cancers. Incretin-based therapies such as GLP-1R agonists have transformed treatment by enhancing insulin secretion, reducing glucagon, and promoting satiety and weight loss. However, their limitations—such as muscle mass loss—highlight the urgent need for more precise strategies.
Signosis offers GPCR/CREB luciferase reporter cell lines that enable monitoring of receptor signaling. These cell models are ideal for studying GLP-1R, GIPR, and Amylin pathways individually or in combination. With the increasing focus on dual receptor agonists, CREB signaling modulation, and small-molecule GLP-1R agonists for oral tablet development, our cell lines provide a powerful and flexible platform for both academic and translational research.
Beyond our standard single-receptor cell lines, Signosis also develops customized dual-receptor reporter models, giving researchers the ability to study receptor crosstalk, synergistic effects, and novel therapeutic mechanisms—key areas for next-generation obesity and diabetes research.
Principle
The GPCR Reporter Stable Cell Lines are engineered using a luciferase-based transcriptional reporter system to enable sensitive, real-time detection of G protein-coupled receptor (GPCR) signaling. These cell lines co-express a specific GPCR of interest along with a luciferase reporter gene driven by a response element responsive to cAMP-mediated downstream signaling pathways.
Upon ligand stimulation, GPCR activation triggers intracellular signaling cascades that lead to the transcriptional activation of the luciferase reporter gene. This system enables dynamic, dose-dependent measurement of receptor activity with low basal signal and a high signal-to-noise ratio. The stable cell lines were established through antibiotic selection and validated for consistent, ligand-specific luciferase induction.
These stable cell lines have been functionally validated using both peptide and non-peptide agonists, demonstrating broad compatibility with diverse ligand classes. This makes them a robust, reproducible platform for high-throughput screening of GPCR modulators, assessment of agonists and antagonists, and detailed pharmacological profiling. These models are ideal for applications in metabolic disease research, neurobiology, immunology, oncology, and beyond.
Ligand binding to GLP1R, GIPR, or the CTR-RAMP3 complex activates Gs-coupled signaling, leading to increased cAMP, PKA activation, and CREB phosphorylation. Phospho-CREB drives transcription of a CRE-luciferase reporter, producing light via firefly luciferase.
G protein-coupled receptor (GPCR)
Luciferase Reporter Cell Lines
GLP-1R Reporter Cell Lines
GIPR Reporter Cell Lines
Amylin3 Reporter Cell Lines
Name | SKU | Price (USD) |
|---|---|---|
Amylin3/CREB Luciferase Reporter HEK293 Stable Cell Line (2 vials) | SL-6003 | $3,870.00 |
Benefits
High Induction
Over 100x Induction delivers clear, measurable responses for confident data interpretation.
Mycoplasma free
Rigorously screened to ensure clean, contamination-free cultures for reliable results.
Ligand-Responsive Readout
Uses the cAMP luciferase system to give a strong, measurable signal only when a ligand activates the receptor.
Mechanism-Focused Research
Helps researchers better understand how specific GIPR isoforms function in different pathways or diseases.
Ready to Use
Stable Cell Lines are immediately ready to use — no extra transfections or optimization needed.
Isoform-Specific Detection
Designed to measure the activity of GPCR, avoiding cross-reactivity seen in traditional assays.
Stable and Reproducible
Stably integrated reporter constructs ensure reproducible performance without the need for repeated transfections.
Fully Validated Performance
Each cell line is tested for correct receptor expression, ligand response, and antibiotic selection.
Fast and Easy Compound Screening
Compatible with both high-throughput and common assay formats, making them ideal for testing drugs or compounds that target GPCR receptors.
Improved Accuracy
Focuses on the receptor’s ligand-binding domain (LBD) instead of the shared DNA-binding region for more precise results.
Broad Agonist Responsiveness
The cell line is functionally validated to respond to both peptide and non-peptide agonists.
We offer a highly sensitive Firefly Luciferase Substrate, which can accurately measure firefly luciferase activity in cells.
Research Applications
Our stable cell lines are developed to support a wide range of discovery and validation studies. They provide a consistent platform for:
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GPCR signaling analysis
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High-throughput compound screening
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Pharmacological profiling
These cell lines help streamline research from early discovery to lead optimization.
