Human PXR Reporter Assay System, 1 x 384-well format assay
Product Overview :
This assay product utilizes proprietary human cells engineered to provide constitutive, high-level expression of the Human Pregnane X Receptor (NR1I2), a ligand-dependent transcription factor commonly referred to as PXR. PXR is also known as the Steroid and Xenobiotic sensing nuclear receptor (SXR).
INDIGO’s Reporter Cells express a hybrid form of human PXR. The N-terminal sequence encoding the PXR DNA binding domain (DBD) has been substituted with that of the yeast GAL4-DBD. The native PXR ligand binding domain (LBD) and other C-terminal domains remain intact and functional. Ligand interaction activates the receptor, causing it to binds to the GAL4 DNA binding sequence, which is functionally linked to a resident luciferase reporter gene. Thus, quantifying changes in luciferase activity in the treated reporter cells provides a sensitive surrogate measure of the changes in PXR activity. The principle application of this reporter assay system is in the screening of test samples to quantify any functional activity, either agonist or antagonist, that they may exert against human PXR.
Pregnane X Receptor is a nuclear receptor that binds and is activated by variety of endogenous and xenobiotic compounds. Activated by the antibiotic rifampicin and various plant metabolites, such as hyperforin, guggulipid, colupulone, and isoflavones, PXR’s response to specific ligands is species-specific. It is activated by naturally occurring steroids, such as pregnenolone and progesterone, and binds to a response element in the promoters of the CYP3A4 and ABCB1/MDR1 genes.
Size : 1 Kit
Shipping : Dry Ice
Stability : Store at -80 degrees; shelf life 180 days maximum after production.
Application(s) : Human
Specificity : Pregnane X Receptor (PXR; NR1I2)
Custom Code : 3822000002
UNSPSC code : 41116104
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