Liver Receptor Homolog-1 (LRH-1; NR5A2)
This nuclear receptor assay system utilizes proprietary non-human mammalian cells engineered to provide high-level expression of a hybrid form of the Human Liver Receptor Homolog-1 (NR5A2), commonly called LRH-1. The N-terminal DNA binding domains (DBD) of the native LRH-1 has been substituted with that of the yeast GAL4-DBD. The reporter gene is beetle luciferase functionally linked to the GAL4 upstream activation sequence (UAS).
As is true in vivo, these reporter cells express LRH-1 that is constitutively active in the (putative) absence of ligand binding. A ligand binding event may diminish the constitutive activity of the receptor (an inverse-agonist response), or further elevates the already high constitutive activity of LRH-1 (an agonist response).
LRH-1 is a nuclear receptor that is an essential regulator of gene transcription, critical for early cellular development and imperative for the proper functions of the liver, pancreas, and intestines during the adult life. In the liver, LRH-1 regulates the expression of key genes involved in bile acid synthesis, cholesterol homeostasis and transport. Because of its decisive role in cell differentiation, LRH-1 is linked to multiple developmental pathways. LRH-1 activity is linked to breast and endometrial cancers as well as intestinal tumors and cancer of the pancreas.
For more information on LRH-1, visit the Nuclear Receptor Resource.
LRH-1 Reporter Cells are prepared using INDIGO’s proprietary CryoMite™ process. This cryo-preservation method yields high cell viability post-thaw, and provides the convenience of immediately dispensing healthy, division-competent reporter cells into assay plates. There is no need for intermediate spin-and-wash steps, viability determinations, or cell titer adjustments.
The principle application of this assay system is in the screening of test samples to quantify agonist and inverse-agonist activities that they may exert against human LRH-1. 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. This kit product is an all-inclusive assay system that includes, in addition to LHR-1 Reporter Cells, two optimized media for use during cell culture and (optionally) in diluting the test samples, a reference agonist, Luciferase Detection Reagent, a cell culture-ready assay plate, and a detailed protocol. All kits are shipped on dry ice.
| Product Family | Product Number | Product Description |
| IB1100 LRH-1 (NR5A2) | IB11001-32 | Human LHR-1 Reporter Assay System, 3 x 32 assays in 96-well format |
| IB11001 | Human LHR-1 Reporter Assay System, 1 x 96-well format assays | |
| IB11002 | Human LHR-1 Reporter Assay System, 1 x 384-well format assays |
Service Assays: Human
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. To initiate a Service Study, download and complete all fields of the Excel worksheet “Service Work Order" then submit the electronic file to INDIGO Customer Service.
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