Dog Pregnane X Receptor (dPXR; nr1i2)
Product Family | Product Number | Product Description | Technical Manual |
D0700 dPXR (nr1i2) |
D07001-32 | Dog PXR Reporter Assay System, 3 x 32 assays in 96-well format | Technical Manual |
D07001 | Dog PXR Reporter Assay System, 1 x 96-well format assays | Technical Manual |
Also available in: Human, Rat, Mouse, Cynomolgus Monkey
This Dog Pregnane X Receptor (dPXR) kit is an all-inclusive assay system that includes, in addition to dPXR Reporter Cells, two optimized media for use during cell culture and in diluting the user’s test samples, a reference agonist, Luciferase Detection Reagent, a cell culture-ready assay plate, and a detailed protocol.
dPXR Reporter Cells are prepared using INDIGO’s proprietary CryoMite™ process. This cryo-preservation method yields exceptional cell viability post-thaw, and provides the convenience of immediately dispensing healthy, division-competent reporter cells into assay plates. There is no need for cumbersome intermediate treatment steps such as spin-and-rinse of cells, viability determinations, or cell titer adjustments prior to assay setup.
INDIGO’s assay kits feature a luciferase detection reagent specially formulated to provide stable light emission between 5 and 90+ minutes after initiating the luciferase reaction. Incorporating a 5-minute reaction-rest period ensures that light emission profiles attain maximal stability, thereby allowing assay plates to be processed in batch. By doing so, the signal output from all sample wells, from one plate to the next, may be directly compared within an experimental set.
Kits are offered in different assay formats to accommodate researchers’ needs: 3x 32 and 1x 96 assay formats for screening small numbers of test compounds, as well as custom bulk reagents for HTS applications.
Bulk assay reagents can be custom manufactured to accommodate any scale of HTS. Please inquire.
Also available in: Human, Rat, Mouse, Cynomolgus Monkey
Pregnane X Receptor also known as nuclear receptor subfamily 1, group I, member 2 (NR1I2) and SXR is a nuclear receptor that binds and is activated by variety of endogenous and xenobiotic compounds. PXR activates the transcription of multiple genes involved in the metabolism and secretion of potentially harmful xenobiotics, drugs, and endogenous compounds. Activated by the antibiotic rifampicin and various plant metabolites, such as hyperforin, guggulipid, colupulone, and isoflavones, its response to specific ligands is species-specific. PXR 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.
This assay product utilizes proprietary mammalian cells engineered to provide constitutive, high-level expression of the Dog 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).
For more information on PXR, visit the Nuclear Receptor Resource.
Service Assays: Human, Rat, Mouse, Cynomologus Monkey, Dog
The primary application of INDIGO’s cell-based nuclear receptor assays are to quantitatively assess the bioactivity of a test compound as an agonist (activator) or antagonist (inhibition of an agonist response) of a given receptor. Service assays include a positive control reference compound and “vehicle” control for every experiment. A formal study report and all data files are provided to the client upon completion of the study. To receive a quote for your proposed study, complete & submit the online “Request a Quote” form or contact an INDIGO Customer Service Representative to discuss your desired study parameters.
Species Differences in Pregnane X Receptor Activation: Examination of common laboratory animal species
INTRODUCTION Nuclear receptors (NRs) are ligand-dependent transcription factors found in many species that regulate the expression of important target genes involved in a spectrum of developmental and physiological processes. In addition to ligand binding, the transcriptional activities of NRs are also modulated through a range of protein-protein interactions with coregulatory proteins, either with coactivator orRead More
Correlation Between Cytochrome P450 Inducers and Nuclear Receptor Activation – a Screening Approach
View Full Size Research conducted by: Shantanu Roychowdhury (1); Casidy M. Ward (1); Kevin J. Kennedy (1); & Yong Zhao (1) (1) Eurofins Discovery, 6 Research Park Drive, St. Charles, MO 63304 Date of Publication: 2019 Presented at: ISSX 2019 in Portland, OR
Intramolecular [2+2] Photocycloaddition of Altrenogest: Confirmation of Product Structure, Theoretical Mechanistic Insight, and Bioactivity Assessment
ABSTRACT While studying the environmental fate of potent endocrine-active steroid hormones, we observed the formation of an intramolecular [2+2] photocycloaddition product (2) with a novel hexacyclic ring system following photolysis of altrenogest (1). The structure and absolute configuration were established by X-ray diffraction analysis. Theoretical computations identified a barrierless two-step cyclization mechanism for the formationRead More
Nuclear Receptors Regulate Intestinal Inflammation in the Context of IBD
ABSTRACT Gastrointestinal (GI) homeostasis is strongly dependent on nuclear receptor (NR) functions. They play a variety of roles ranging from nutrient uptake, sensing of microbial metabolites, regulation of epithelial intestinal cell integrity to shaping of the intestinal immune cell repertoire. Several NRs are associated with GI pathologies; therefore, systematic analysis of NR biology, the underlyingRead More
Rifamycin SV exhibits strong anti-inflammatory in vitro activity through pregnane X receptor stimulation and NFkB inhibition
ABSTRACTRifamycin SV (rifamycin), is a member of the ansamycin family of antimicrobial compounds which kills bacteria commonly associated with infectious diarrhea and other enteric infections. Rifamycin has been found to be effective in experimental animal models of gut inflammation and its efficacy in these settings has been attributed partially to immunomodulatory non-bactericidal activities. This studyRead More
Sedaxane—Use of Nuclear Receptor Transactivation Assays, Toxicogenomics, and Toxicokinetics as Part of a Mode of Action Framework for Rodent Liver Tumors
ABSTRACT Experimental data demonstrate a mode of action (MOA) for liver tumors in male rats and mice treated with sedaxane that starts with activation of CAR, followed by altered expression of CAR-responsive genes, increased cell proliferation, and eventually clonal expansion of preneoplastic cells, leading to the development of altered foci and tumors. This MOA isRead More
Profiling Drug Activity of Human and Ortholog Xenobiotic-Sensing Receptors: PXR, CAR, AhR, and FXR
View Full Size Research conducted by: Koji Toyokawa (1), Ewa Maddox (1), Jack Vanden Huevel (1,2), & Bruce Sherf (1) (1) INDIGO Biosciences, Inc., 1981 Pine Hall Rd, State College, PA, USA (2) Center for Molecular Toxicology and Carcinogenesis, 325 Life Sciences Building, Penn State University, University Park, PA 16802, USA Date of Publication: 2017
Mouse Liver Tumor Mode of Action: Use of Toxicogenomics in Weight of Evidence for Human Relevance Assessment
ABSTRACT The Use of Toxicogenomics in Chemical Safety Testing Current safety testing is geared to produce and accept descriptive data from high-dose animal studies Interpretation of this information has effectively protected our health and safety for decates; however, hindered by lack of understanding mechanistic information Concern over chemical safety for humans and the environment hasRead More
Species Differences in Pregnane X Receptor Activation: Examination of common laboratory animal species
ABSTRACT Nuclear receptors (NRs) are ligand-dependent transcription factors found in many species that regulate the expression of important target genes involved in a spectrum of developmental and physiological processes. The ligand binding domain (LBD) of NRs is responsible for both ligand recognition and regulation of protein-protein interactions, notably with coregulatory factors. NRs represent important targetsRead More
INDIGO Offers Next Generation in PXR Assay Systems
Expansion of Assay Critical to the Study of Metabolism and Drug-Drug Interactions State College, PA (June 7, 2016) INDIGO Biosciences, a recognized industry-leading provider of nuclear receptor products and services, announced today that it has completed development of the next generation of Pregnane X Receptor (PXR) technology. Previously available in kits and services for onlyRead More