Puracyp - Nuclear Receptor Activation Kits
Puracyp’s nuclear receptor activation kits are all-inclusive cell-based assay systems. The kits incorporate mycoplasm-free, stably-transfected cells derived from hepatoma cell lines that have been treated with a cell-arrest agent to prevent further proliferation. Exposure to the cell-arrest agent ensures that the cells in the kits can only be used for a single 96 well assay. Each kit includes the stably integrated receptor and reporter cells.
The kits also include a cell culture-ready assay plate, optimized cell culture media, cell dosing media, a positive control specific for the nuclear receptor, CellTiter-Fluor™ for determining cell viability, luciferase detection reagents and, if so ordered, a P450-Glo™ substrate for assessing induction of CYP450 enzyme activity. Also included in the kits are a detailed Technical Manual and a Protocol Quick Guide. Further details on the use of CellTiter-Fluor™, ONE-Glo™ and the P450-Glo™ CYP3A4 or CYP1A2 Assay with Luciferin-IPA can be found at www.promega.com. The primary application of these assay kits is to identify agents with the ability to activate PXR and/or AhR, thereby inducing drug-metabolizing enzymes and ABC transporters.
Catalog Number: Description
- DPX2-96-001: Human PXR activation and cell viability in 96 well format
- DPX2-96-002: Human PXR activation and cell viability with CYP3A metabolism in 96 well format
- DRE-1A2-96-001: Human AhR activation and cell viability in 96 well format
- RPXR-96-001: Rat PXR activation and cell viability in 96 well format
- RPXR-96-002: Rat PXR activation and cell viability with CYP3A metabolism in 96 well format
- hCAR1-96-001: Human CAR1 activation and cell viability in 96 well plate
- hCAR3-96-001: Human CAR3 activation and cell viability in 96 well plate
Employing reporter genes governed by the P450 promoters allows for accurate gene activation from the ligand-activated receptor. Correlations between binding affinity and activation are more readily predicted.
When ligands bind to the full-length receptor they can produce conformational alterations that influence the extent of gene transcription. Our competitors employ only the ligand binding domain (LBD) of the receptor.
Low variability and high reproducibility with results comparable to those obtained in primary cultures.,Simple and easy to perform, with completion in 24 to 48 hours.,Indirect NR activators can be identified. Indirect activators cannot be detected with mammalian two-hybrid or ligand binding assays.,Puracyp is the only nuclear receptor (NR) company that has functional assays allowing agonists to be differentiated from antagonist. Our competitors assays only determine binding to the LBD. These assays cannot identify agonism vs antagonism.