Rat Peroxisome Proliferator-Activated Receptor Alpha (rPPARα; nr1c1)
|Product Family||Product Number||Product Description||Technical Manual|
|R00111-32||Rat PPARα Reporter Assay System, 3 x 32 assays in 96-well format||Technical Manual|
|R00111||Rat PPARα Reporter Assay System, 1 x 96-well format assays||Technical Manual|
Kits are offered in different assay formats to accommodate researchers’ needs: 3x 32 and 1x 96-well assay formats for screening small numbers of test compounds, as well as custom bulk reagents for HTS applications. Assay systems are all inclusive, providing reporter cells, optimized growth media, media for diluting test compounds, a positive-control agonist, luciferase detection reagent, a white assay plate, a detailed protocol, and a protocol quick guide. All kits are shipped on dry ice.
rPPARα 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.
This kit product is an all-inclusive assay system that includes, in addition to rPPARα 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.
Bulk assay reagents can be custom manufactured to accommodate any scale of HTS. Please inquire.
INDIGO’s Rat PPAR alpha (nr1c1; pparA; rPPARα) Assay utilizes proprietary rodent cells engineered to provide high-level expression of rPPARα. Reporter Cells also incorporate a responsive luciferase reporter gene, therefore, quantifying expressed luciferase activity provides a sensitive surrogate measure of rPPARα activity in the treated cells. The principle application of this reporter assay system is in the screening of test samples to quantify functional activity, either agonist or antagonist, that they may exert against rat PPARα.
For more information on PPARα, visit the Nuclear Receptor Resource.
Service Assays: Human, Mouse, Rat, Cyn 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.
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Discovery of potent and selective PPARα/δ dual antagonists and initial biological studies Author links open overlay panel
ABSTRACT We previously published on the design and synthesis of novel, potent and selective PPARα antagonists suitable for either i.p. or oral in vivo administration for the potential treatment of cancer. Described herein is SAR for a subsequent program, where we set out to identify selective and potent PPARα/δ dual antagonist molecules. Emerging literature indicates that both
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ABSTRACT Small molecule agonism of PPARα represents a promising new avenue for the development of non-invasive treatments for oculovascular diseases like diabetic retinopathy and age-related macular degeneration. Herein we report initial structure–activity relationships for the newly identified quinoline-based PPARα agonist, Y-0452. Preliminary computational studies led to the hypothesis that carboxylic acid transposition and deconstruction of
ABSTRACT The invention disclosed herein is directed to compounds of Formula I and pharmaceutically acceptable salts thereof, which are useful in the treatment of prostate, breast, colon, pancreatic, human chronic lymphocytic leukemia, acute or chronic myeloid leukemia, melanoma, and other cancers. The invention also includes pharmaceutical compositions comprising a therapeutically effective amount of compound of
Sedaxane—Use of Nuclear Receptor Transactivation Assays, Toxicogenomics, and Toxicokinetics as Part of a Mode of Action Framework for Rodent Liver Tumors
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GPR40 partial agonist MK-2305 lower fasting glucose in the Goto Kakizaki rat via suppression of endogenous glucose production
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ABSTRACT The invention disclosed herein is directed to compounds of Formula (1a) and (1b) and pharmaceutically acceptable salts thereof, which are useful in the treatment of prostate, breast, colon, pancreatic, human chronic lymphocyticδ leukemia, melanoma and other cancers. The invention also comprises pharmaceutical compositions comprising a therapeutically effective amount of compound of Formula (1a) or