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CB1R Reporter Assay Kit
Product Description and Product Data
This is an all-inclusive cell-based luciferase reporter assay kit targeting the Human Cannabinoid Type 1 Receptor (CB1R). INDIGO’s CB1R reporter assay utilizes proprietary mammalian cells that have been engineered to provide constitutive expression of Human Cannabinoid Type 1 Receptor. In addition to CB1R Reporter Cells, this kit provides two optimized media for use during cell culture and in diluting the user’s test samples, a reference agonist, Luciferase Detection Reagent, and a cell culture-ready assay plate. The principal application of this assay is in the screening of test samples to quantify any functional activity, either agonist or antagonist, that they may exert against human CB1R. This kit provides researchers with clear, reproducible results, exceptional cell viability post-thaw, and consistent results lot to lot. Kits must be stored at -80C. Do not store in liquid nitrogen. Note: reporter cells cannot be refrozen or maintained in extended culture.
Features
Clear, Reproducible Results
- All-Inclusive Assay Systems
- Exceptional Cell Viability Post-Thaw
- Consistent Results Lot to Lot
Product Specifications
| Target Type | GPCR | ||
| Species | Human | ||
| Receptor Form | Native | ||
| Assay Mode | Agonist, Antagonist | ||
| Kit Components |
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| Shelf Life | 6 months | ||
| Orthologs Available | No | ||
| Shipping Requirements | Dry Ice | ||
| Storage temperature | -80C |
Data
Target Background
The Cannabinoid Type 1 Receptor is one of the two main cannabinoid receptors identified as part of the endocannabinoid system. The CB1 Receptor is highly expressed in the central nervous system, but also in skeletal muscles, gastrointestinal tract, liver, pancreas, skin, reproductive system, and cardiovascular system. The Cannabinoid Type 1 Cannabinoid Receptor is involved in a wide range of physiological and pathophysiological processes related to neurological disorders, energy metabolism, obesity, diabetes, cardiovascular and reproductive disorders, inflammation, and cancer.
The CB1 Receptor is a member of the super-family of G protein-coupled receptors (GPCR). Its structure includes seven transmembrane helices, with an extracellular amino end and an intracellular carboxy tail associated with trimeric G proteins. Upon ligand binding, the receptor undergoes conformational change that triggers the activation of G proteins via an exchange of GDP to a GTP.
Modes of Cannabinoid Type 1 Cannabinoid Receptor signal transduction are diverse and may involve a variety of signaling molecules and kinases that vary based on the type of ligand and the type of cells in which the receptor is expressed. The first signaling pathway described for CB1 receptors involved activation of a pertussis toxin sensitive G protein (Gαi/o), leading to the inhibition of forskolin-stimulated cyclic AMP, activation of G protein-coupled inwardly rectifying potassium channels (GIRKs), and an inhibition of several calcium channels. This is followed by recruitment of β-arrestin, a cytosolic protein involved in receptor desensitization and internalization. However, β-arrestin activation is also involved in the activation of downstream kinases such as MAPK.
CB1R can also couple with stimulatory G proteins such as Gαs and Gαq/11, resulting in the activation of ERK and PLC pathways and increased levels of intracellular calcium. An outcome of CB1R activation is that calcineurin, a calcium-dependent phosphatase, dephosphorylates and activates the transcription factor NFAT. Signal transduction via the Ca+2-calcineurin / NFAT cascade is exploited by the reporter cells used in this assay.
This CB1 Cannabinoid Reporter assay uses proprietary human cells that provide constitutive expression of the Human Cannabinoid Type 1 Receptor.
INDIGO’s CB1 Cannabinoid Receptor Reporter Cells contain an engineered luciferase reporter gene functionally linked to tandem NFAT genetic response elements (GRE) and a minimal promoter. Activated NFAT binds to its corresponding GREs to initiate the formation of a complete transcription complex that drives Luc gene expression. Quantifying changes in luciferase activity in the treated reporter cells relative to the untreated cells provides a sensitive, dose-dependent surrogate measure of drug-induced changes in CB1 Cannabinoid Receptor activity. Accordingly, the principal application of this reporter assay is in the screening of test compounds to quantify any functional activities, either activating or inhibitory, that they may exert against CB1R or its associated calcineurin-NFAT signal transduction pathway.
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