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  • HOME
  • ABOUT
    • About
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    • Ortholog Assays
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    • In Vitro Toxicology Platform
    • MDR1 / Human P-Glycoprotein
    • Gene Expression
    • NASH Nuclear Receptors For Research
    • Disease States
    • Live Cell Multiplex
    • Custom Assay Development
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Aryl Hydrocarbon Receptor (AhR)

Product Family Product Number Product Description Technical Manual
IB0600
AhR
IB06001-32 Human AhR Reporter Assay System, 3 x 32 assays in 96-well format Technical Manual
IB06001 Human AhR Reporter Assay System, 1 x 96-well format assays Technical Manual
IB06002 Human AhR Reporter Assay System, 1 x 384-well format assays

Aryl Hydrocarbon Receptor (AhR)

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Also available in: Human, Rat, Zebrafish

This Human Aryl Hydrocarbon Receptor (AhR) assay kit is an all-inclusive system which includes in addition to AhR Reporter Cells, two optimized media for use during cell culture and in diluting the user’s test samples, a reference agonist (MeBIO), Luciferase Detection Reagent, and a cell culture-ready assay plate.

AhR 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, cell titer adjustments, or the pre-incubation of reporter cells 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.

Aryl Hydrocarbon Receptor Agonist and Antagonist

Assay Kit & Platforms

Bulk assay reagents can be custom manufactured to accommodate any scale of HTS. Please inquire.

Also available in: Human, Rat, Zebrafish

Although technically not a member of the Nuclear Receptor (NR) superfamily, the AhR shares many of the same attributes. The AhR is a member of the basic helix-loop-helix, Per-Arnt-Sim (bHLH-PAS) family of transcription factors and is responsible for the toxicologic effects of 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD, often referred to as simply “dioxin”) and several other related polycyclic aromatic hydrocarbons. The basic mechanism of action of dioxin and related compounds has been extensively studied, in particular as it relates to regulation of cytochrome P450 1A1 (CYP1A1).

AhR is present in most cell types and in the unactivated state is cytosolic and exists in a complex with chaperone proteins such as heat shock protein 90 (Hsp90). Binding of TCDD and related molecules to AhR leads to nuclear translocation and heterodimerization with its partner protein ARNT, another bHLH-PAS family member. The AhR-ARNT heterodimer binds to specific cognate DNA sequence elements known as dioxin/xenobiotic response elements (DRE/XRE) present in the regulatory region of specific genes such as CYP1A1. Binding of the AhR:ARNT heterodimer to these elements, and subsequent recruitment of transcription coactivator complexes, leads to increased transcription of the specific gene, known as “target genes.” There is a battery of genes affected in this manner and targets include certain xenobiotic-metabolizing enzymes, such as CYP1A1,CYP1A2, CYP2B1, and UGT1A6. In addition, genes affected directly and indirectly by the TCDD/AhR-complex code for both inhibitory and stimulatory growth factors and their gene products affect cellular growth and differentiation leading to tumor promotion and carcinogenicity as well as other forms of toxicity.

INDIGO’s Aryl Hydrocarbon Receptor (AhR) Assay is a cell-based genetic reporter assay that utilizes the luciferase reporter gene Aryl Hydrocarbon Receptor Agonist and Antagonist Assays functionally linked to an AhR-responsive promoter. Thus, quantifying changes in luciferase expression in the treated reporter cells provides a sensitive surrogate measure of the changes in AhR 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 AhR.

For more information on AhR, visit the Nuclear Receptor Resource.

Service Assays: Human, Rat, Zebrafish

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.

Xenobiotic Metabolism; Bile Acid and Xenobiotic; Toxicology; Drug-Nutrient Interaction; Environmental Toxicology

Breastmilk-promoted bifidobacteria produce aromatic lactic acids in the infant gut

ABSTRACT Breastfeeding profoundly shapes the infant gut microbiota, which is critical for early life immune development. However, few breastmilk-dependent microbial metabolites mediating host-microbiota interactions are currently known. We here demonstrate that breastmilk-promoted Bifidobacterium species convert aromatic amino acids (tryptophan, phenylalanine and tyrosine) into their respective aromatic lactic acids (indolelactate, phenyllactate and 4-hydroxyphenyllactate) via a previouslyRead More

Posted in New Publications | Tagged AhR, aryl hydrocarbon receptor | Comments Off on Breastmilk-promoted bifidobacteria produce aromatic lactic acids in the infant gut

Quinazolinone derivative BNUA‐3 ameliorated [NDEA+2‐AAF]‐ induced liver carcinogenesis in SD rats by modulating AhR‐CYP1B1‐Nrf2‐Keap1 pathway

ABSTRACT Cytochrome P450 1B1, considered as one of the novel chemotherapeutic targets involved in cancer prevention and therapy is also associated with the conversion of procarcinogens into their active metabolites. The aryl hydrocarbon receptor (AhR) is responsible for mediating different biological responses to a wide variety of environmental pollutants and also causes transcriptional activation ofRead More

Posted in New Publications | Tagged AhR, CYP1B1, FESEM, hepatocellular carcinogenesis, NDEA+ 2-AAF, ortholog, SD rats | Comments Off on Quinazolinone derivative BNUA‐3 ameliorated [NDEA+2‐AAF]‐ induced liver carcinogenesis in SD rats by modulating AhR‐CYP1B1‐Nrf2‐Keap1 pathway

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

Posted in New Publications, Posters | Tagged AhR, CAR, cyp450 inducer, cytochrome p450, PXR | Comments Off on Correlation Between Cytochrome P450 Inducers and Nuclear Receptor Activation – a Screening Approach

Enhancement of the gut barrier integrity by a microbial metabolite through the Nrf2 pathway

ABSTRACT The importance of gut microbiota in human health and pathophysiology is undisputable. Despite the abundance of metagenomics data, the functional dynamics of gut microbiota in human health and disease remain elusive. Urolithin A (UroA), a major microbial metabolite derived from polyphenolics of berries and pomegranate fruits displays anti-inflammatory, anti-oxidative, and anti-ageing activities. Here, weRead More

Posted in New Publications | Tagged AhR, gut microbiota, Nrf2, UAS03, UroA, Urolithin A | Comments Off on Enhancement of the gut barrier integrity by a microbial metabolite through the Nrf2 pathway

Differential and Overlapping Effects of 20,23(OH)2D3 and 1,25(OH)2D3 on Gene Expression in Human Epidermal Keratinocytes: Identification of AhR as an Alternative Receptor for 20,23(OH)2D3

ABSTRACT A novel pathway of vitamin D activation by CYP11A has previously been elucidated. To define the mechanism of action of its major dihydroxy-products, we tested the divergence and overlap between the gene expression profiles of human epidermal keratinocytes treated with either CYP11A1-derived 20,23(OH)2D3 or classical 1,25(OH)2D3. Both secosteroids have significant chemical similarity with theRead More

Posted in New Publications | Tagged AhR, dihydroxyvitamin D, epidermal keratinocytes, microarray, nuclear receptor signaling, Vitamin D | Comments Off on Differential and Overlapping Effects of 20,23(OH)2D3 and 1,25(OH)2D3 on Gene Expression in Human Epidermal Keratinocytes: Identification of AhR as an Alternative Receptor for 20,23(OH)2D3

Metadichol, A Novel ROR Gamma Inverse Agonist and Its Applications in Psoriasis

ABSTRACT Psoriasis affects 3% of the population worldwide, and there is no known cure. Psoriasis is associated with an increased risk of psoriatic arthritis, lymphomas, cardiovascular disease, and Crohn’s disease. Psoriasis treatments today include steroid and vitamin D3 cream, ultraviolet light, and immune system suppressing medications such as methotrexate. The T cells responsible for psoriasisRead More

Posted in New Publications | Tagged AhR, inverse agonist, psoriasis, ROR, RORC, RORg, RORγ, TNF alpha, VDR, Vitamin D | Comments Off on Metadichol, A Novel ROR Gamma Inverse Agonist and Its Applications in Psoriasis

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

Posted in New Publications | Tagged AhR, CAR, constitutive androstane receptor, liver tumor, ortholog, PPARa, PPARα, PXR, sedaxane | Comments Off on Sedaxane—Use of Nuclear Receptor Transactivation Assays, Toxicogenomics, and Toxicokinetics as Part of a Mode of Action Framework for Rodent Liver Tumors

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

Posted in New Publications, Posters | Tagged AhR, CAR, drug activity, FXR, ortholog, PXR, SOT 2017 | Comments Off on Profiling Drug Activity of Human and Ortholog Xenobiotic-Sensing Receptors: PXR, CAR, AhR, and FXR

Indigo Announces In Vitro Toxicology Platform

In vitro toxicology platform provides predictive model of liver toxicity.  Aims to reduce the high rates of drug­-induced liver damage State College, PA (May 4, 2016) INDIGO Biosciences, the recognized industry leader in nuclear receptor research, has completed development of an in vitro toxicology platform, meeting the demand for predictive liver toxicity models.  INDIGO’s inRead More

Posted in press | Tagged AhR, CAR, In Vitro Toxicology, LRH-1, LXR, Nrf2, PPAR, PXR | Comments Off on Indigo Announces In Vitro Toxicology Platform

Triphenyl phosphate-induced developmental toxicity in zebrafish: Potential role of the retinoic acid receptor

ABSTRACT Using zebrafish as a model, we previously reported that developmental exposure to triphenyl phosphate (TPP) – a high-production volume organophosphate-based flame retardant – results in dioxin-like cardiac looping impairments that are independent of the aryl hydrocarbon receptor. Using a pharmacologic approach, the objective of this study was to investigate the potential role of retinoicRead More

Posted in New Publications | Tagged AhR, RAR | Comments Off on Triphenyl phosphate-induced developmental toxicity in zebrafish: Potential role of the retinoic acid receptor
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