Rat Peroxisome Proliferator-Activated Receptor Delta (rPPARδ; nr1c2)
|Product Family||Product Number||Product Description||Technical Manual|
|R00121-32||Rat PPARδ Reporter Assay System, 3 x 32 assays in 96-well format||Technical Manual|
|R00121||Rat PPARδ 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.
rPPARδ 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 rPPARδ 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 delta (nr1c2; pparD/B; rPPARδ) Assay utilizes proprietary rodent cells engineered to provide high-level expression of rPPARδ. Reporter Cells also incorporate a responsive luciferase reporter gene, therefore, quantifying expressed luciferase activity provides a sensitive surrogate measure of rPPARδ 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 PPARδ.
For more information on PPARδ, 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. 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.
GPR40 partial agonist MK-2305 lower fasting glucose in the Goto Kakizaki rat via suppression of endogenous glucose production
ABSTRACT GPR40 (FFA1) is a fatty acid receptor whose activation results in potent glucose lowering and insulinotropic effects in vivo. Several reports illustrate that GPR40 agonists exert glucose lowering in diabetic humans. To assess the mechanisms by which GPR40 partial agonists improve glucose homeostasis, we evaluated the effects of MK-2305, a potent and selective partial
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
Design, synthesis, and biological evaluation of novel thiazolidinediones as PPARγ/FFAR1 dual agonists
ABSTRACT Diabetes mellitus is a chronic metabolic disorder that affects more than 180 million people worldwide. Peroxisome proliferator activated receptors (PPARs) are a group of nuclear receptors that have been targeted by the thiazolidinedione (TZD) class of compounds for the management of type II diabetes. PPARγ is known to regulate adipogenesis and glucose metabolism. Another
Systems toxicology identifies mechanistic impacts of 2-amino-4,6-dinitrotoluene (2A-DNT) exposure in Northern Bobwhite
ABSTRACT Background: A systems toxicology investigation comparing and integrating transcriptomic and proteomic results was conducted to develop holistic effects characterizations for the wildlife bird model, Northern bobwhite (Colinus virginianus) dosed with the explosives degradation product 2-amino-4,6-dinitrotoluene (2A-DNT). A subchronic 60d toxicology bioassay was leveraged where both sexes were dosed via daily gavage with 0, 3, 14, or 30 mg/kg-d
Keratinocyte differentiation and upregulation of ceramide synthesis induced by an oat lipid extract via the activation of PPAR pathways
ABSTRACT Activation of peroxisome proliferator-activated receptors (PPARs) has been shown to have an important role in skin barrier function by regulating differentiation and lipid synthesis in keratinocytes. Oat (Avena sativa) has long been used as a soothing agent to relieve skin irritations, and the clinical benefits of topical oat formulations have been proven; however, the
ABSTRACT The RAR-related orphan receptor gamma t (RORγt) is a nuclear receptor required for generating IL-17–producing CD4+ Th17 T cells, which are essential in host defense and may play key pathogenic roles in autoimmune diseases. Oxysterols elicit profound effects on immune and inflammatory responses as well as on cholesterol and lipid metabolism. Here, we describe the identification of several naturally occurring
ABSTRACT Omega-3-PUFAs, eicosapentaenoic acid (EPA), and docosahexaenoic acid (DHA), are associated with prevention of various aspects of metabolic syndrome. In the present studies, the effects of oil rich in EPA on gene expression and activation of nuclear receptors was examined and compared with other 3-PUFAs. The EPA-rich oil (EO) altered the expression of FA metabolism genes in THP-1 cells, including stearoyl
ABSTRACT PPARa L162A, PPARg 12A, PPARβ/d rs226766 , and PGC-1a G482S genotype distributions were compared with TFEQ-R18 and ecSI scores; responses were gender-specific and paralleled published values. Results confirmed less emotional eating (EE) (P<.001), cognitive restraint (CR) (P<.001) and uncontrolled eating (UE) (P=.1) with EC (ecSI score >= 32). Subjects in the lowest ecSI tertile
Differential Activation of Nuclear Receptors by Perflunoriated Fatty Acid Analogs and Natural Fatty Acids: A Comparison of Human, Mouse, and Rat Peroxisome Proliferator-Activated Receptor Receptor-a, -b, and -c, Liver X Receptor-b, and Retinoid X Receptor-a
ABSTRACT Administration of ammonium salts of perfluorooctanoate (PFOA) to rats results in peroxisome proliferation and benign liver tumors, events associated with activation of the nuclear receptor (NR) peroxisome proliferator-activated receptor-a (PPARa). Due to its fatty acid structure, PFOA may activate other NRs, such as PPARb, PPARg, liver X receptor (LXR), or retinoid X receptor (RXR). In this study, the