• ABOUT
    • About INDIGO
    • Why INDIGO
    • Key Personnel
      • Board of Directors & Advisors
      • Management
    • Employment
    • INDIGO Press Releases
    • INDIGO in the News
  • ASSAYS
    • By Receptor
    • By Disease State
      • Overview
      • Anemia & Kidney Disease
      • Autoimmune Disease & Inflammation
      • Cancer
      • Cardiovascular Disease
      • Diabetes
      • Endocrinology
      • NAFLD/NASH
      • Obesity
    • Toxicology Solutions
      • In Vitro Toxicology Platform
      • Gene Expression
      • MDR1 / Human P-Glycoprotein
      • Discovery Toxicology
      • Environmental Monitoring
    • INDIGlo Luciferase Detection Reagent
    • Live Cell Multiplex
    • Ortholog Assays
    • Custom Assay Development
  • TECHNOLOGY
    • Nuclear Receptor Overview
    • Assay Kit Platform & Formats
    • Nuclear Receptor Profiling & Panels
    • Environmental Testing Solutions
    • Growth Factor Receptors
    • upcyte® Hepatocytes
    • FAQ
  • RESOURCES
    • Technical Manuals
    • Safety Data Sheets
    • Scientific Whitepapers from INDIGO
    • Scientific Posters
    • New Research Publications
    • Nuclear Receptor Resource
  • CONTACT US
    • Contact INDIGO
    • Request a Quote
    • Request Information
    • Distributors
    • Terms & Conditions
      • Product Policies
      • Limited Use Disclosures
  • BLOG
Search site...

± α β γ δ Δ ε ζ κ ω ö ® ™ µ

  • ABOUT
    • About INDIGO
    • Why INDIGO
    • Key Personnel
      • Board of Directors & Advisors
      • Management
    • Employment
    • INDIGO Press Releases
    • INDIGO in the News
  • ASSAYS
    • By Receptor
    • By Disease State
      • Overview
      • Anemia & Kidney Disease
      • Autoimmune Disease & Inflammation
      • Cancer
      • Cardiovascular Disease
      • Diabetes
      • Endocrinology
      • NAFLD/NASH
      • Obesity
    • Toxicology Solutions
      • In Vitro Toxicology Platform
      • Gene Expression
      • MDR1 / Human P-Glycoprotein
      • Discovery Toxicology
      • Environmental Monitoring
    • INDIGlo Luciferase Detection Reagent
    • Live Cell Multiplex
    • Ortholog Assays
    • Custom Assay Development
  • TECHNOLOGY
    • Nuclear Receptor Overview
    • Assay Kit Platform & Formats
    • Nuclear Receptor Profiling & Panels
    • Environmental Testing Solutions
    • Growth Factor Receptors
    • upcyte® Hepatocytes
    • FAQ
  • RESOURCES
    • Technical Manuals
    • Safety Data Sheets
    • Scientific Whitepapers from INDIGO
    • Scientific Posters
    • New Research Publications
    • Nuclear Receptor Resource
  • CONTACT US
    • Contact INDIGO
    • Request a Quote
    • Request Information
    • Distributors
    • Terms & Conditions
      • Product Policies
      • Limited Use Disclosures
  • BLOG
Print Friendly, PDF & Email

Constitutive Androstane Receptor-1 (CAR-1; NR1I3i1)

Assay available as Screening Service

  • Services
  • Background
  • Data
  • Research Areas

Constitutive Androstane Receptor-1 Assay Services

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.

CAR-1 Service Assays: Human,Mouse

Constitutive Androstane Receptor-1 Background

Human Constitutive Androstane Receptor-1 (CAR-1) exhibits constitutive activity, but can be further regulated through direct ligand interactions. The primary application of this reporter assay system is in the screening of test samples to quantify any functional inverse-agonist activity that they may exert on human CAR-1. INDIGO’s CAR-1 Reporter Assay System utilizes proprietary mammalian cells engineered to provide high-level expression of human CAR-1 (NR1I3 isoform 1), which is a constitutively active transcription factor.

Reporter Cells utilize a modified version of human CAR1 in which the N-terminal DNA binding domain (DBD) has been replaced with the GAL4-DBD. The human CAR1 ligand binding domain (LBD) is unaltered and fully functional. These reporter cells also incorporate a luciferase cDNA functionally linked to the GAL4-upstream activation sequence (UAS). Thus, quantifying expressed luciferase activity provides a sensitive surrogate measure of changes in CAR1 activity resulting from a direct interaction between a treatment compound and the nuclear receptor. Because this assay system expresses a GAL4-DBD + hCAR1 LBD hybrid receptor, the bio-activity of activators that act through indirect mechanisms (such as those that alter the phosphorylation status of the native N-terminal amino acid sequence of CAR1) may be dampened or go undetected.

CAR is encoded by the NR1I3 gene. This gene encodes a member of the nuclear receptor superfamily, and is a key regulator of xenobiotic and endobiotic metabolism. The protein binds to DNA as a monomer or a heterodimer with the retinoid X receptor and regulates the transcription of target genes involved in drug metabolism and bilirubin clearance, such as cytochrome P450 family members. Unlike most nuclear receptors, this transcriptional regulator is constitutively active in the absence of ligand but is regulated by both agonists and inverse agonists. Ligand binding results in translocation of this protein to the nucleus, where it activates or represses target gene transcription. These ligands include bilirubin, a variety of foreign compounds, steroid hormones, and prescription drugs.

The principle application of this assay product is in the screening of test samples to quantify functional inverse-agonist activities that they may exert against the human constitutive androstane receptor.

Synonyms:Constitutive Androstane Receptor-1, CAR-1, NR1I3i1

Constitutive Androstane Receptor-1 Assay Data

constitutive androstane receptor-1 inverse-agonist

Constitutive Androstane Receptor-1 Assay Research Areas

Xenobiotic Metabolism; Bile Acid and Xenobiotic Metabolism; Toxicology; NAFLD/NASH

Research articles associated with CAR

Request a Quote Icon
Search site...
Click to Insert Symbols in Search

α β γ δ Δ ε ζ κ ® ™ µ

Want More Information?

Resource Quick Links

  • Technical Manuals & Product Listing
  • Safety Data Sheets
  • Sample Study Report
  • Study Work Order Form

3006 Research Drive, Suite A1, State College, PA, USA 16801

+1 (814) 234-1919

  • Home
  • Products
  • Request a Quote
  • FAQ

© 2022 INDIGO Biosciences, Inc. All Rights Reserved