Zebrafish Peroxisome Proliferator-Activated Receptor Gamma (zPPARγ; nr1c3)
|Product Family||Product Number||Product Description||Technical Manual|
|Z00101-32||Zebrafish PPARγ Reporter Assay System, 3 x 32 assays in 96-well format||Technical Manual|
|Z00101||Zebrafish PPARγ Reporter Assay System, 1 x 96-well format assays||Technical Manual|
Zebrafish Peroxisome Proliferator-Activated Receptor Gamma Assay Kit
This Zebrafish Peroxisome Proliferator Activated Receptor Gamma (zPPARγ) assay kit is an all-inclusive firefly luciferase reporter assay system that includes in addition to zPPARγ 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.
zPPARγ 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.
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.
Bulk assay reagents can be custom manufactured to accommodate any scale of HTS. Please inquire.
PPARg assay kits also available in: Human, Rat/Mouse Shared Ortholog, Cyn Monkey
Zebrafish Peroxisome Proliferator-Activated Receptor Gamma 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.
Service Assays: Human, Rat/Mouse Shared Ortholog, Cyn Monkey, Zebrafish
Zebrafish Peroxisome Proliferator-Activated Receptor Gamma Assay Background
Peroxisome proliferator-activated receptor gamma (PPAR-gamma or PPARγ), also known as the glitazone receptor, or NR1C3 (nuclear receptor subfamily 1, group C, member 3) is a type II nuclear receptor that in humans is encoded by the PPARG gene. PPARs form heterodimers with retinoid X receptors (RXRs) and these heterodimers regulate transcription of various genes. PPARγ regulates adipocyte differentiation, fatty acid storage and glucose metabolism. The PPARγ knockout mice fail to generate adipose tissue when fed a high fat diet. Many insulin sensitizing drugs used in the treatment of diabetes target PPARγ as a means to lower serum glucose without increasing pancreatic insulin secretion. Additionally, PPARγ has been implicated in the pathology of numerous diseases including obesity, diabetes, atherosclerosis and cancer. Alternatively spliced transcript variants that encode different isoforms have been described.
INDIGO’s Zebrafish Peroxisome Proliferator Activated Receptor Gamma Reporter Assay System utilizes proprietary mammalian cells engineered to provide constitutive, high-level expression of Zebrafish (Danio rerio) PPARγ (nr1c3), a ligand-dependent transcription factor.
INDIGO's Reporter Cells include the luciferase reporter gene functionally linked to an zPPARγ-responsive promoter. Thus, quantifying changes in luciferase expression in the test sample-treated reporter cells provides a sensitive surrogate measure of changes in zPPARγ activity. The principal application of this assay is in the screening of test samples to quantify any functional bioactivity that they may exert against zebrafish PPARγ. In particular, zebrafish reporter assays are frequently used in the monitoring of environmental samples for the presence of biohazardous chemical pollutants, such as endocrine disruptors.
For more information on PPARγ, visit the Nuclear Receptor Resource.
Zebrafish Peroxisome Proliferator-Activated Receptor Gamma Assay Research Areas
Lipoxygenase catalyzed metabolites derived from docosahexaenoic acid are promising antitumor agents against breast cancer
ABSTRACT Docosahexaenoic acid (DHA) is known to inhibit breast cancer in the rat. Here we investigated whether DHA itself or select metabolites can account for its antitumor action. We focused on metabolites derived from the lipoxygenase (LOX) pathway since we previously showed that they were superior anti-proliferating agents compared to DHA; 4-OXO-DHA was the most
ABSTRACT Gastrointestinal (GI) homeostasis is strongly dependent on nuclear receptor (NR) functions. They play a variety of roles ranging from nutrient uptake, sensing of microbial metabolites, regulation of epithelial intestinal cell integrity to shaping of the intestinal immune cell repertoire. Several NRs are associated with GI pathologies; therefore, systematic analysis of NR biology, the underlying
Structures and biological activities of new carnosic acid- and carnosol-related compounds generated by heat treatment of rosemary
ABSTRACTCarnosic acid (CA) and carnosol (CS) are components of rosemary reported to possess antioxidative and peroxisome proliferator-activated receptor gamma (PPARγ) transcriptional activities that are useful for preventing metabolic disorders. The aims of this study were to identify new bioactive compounds in heated rosemary and examine their effects on antioxidative stress and PPARγ activation. In heated
ABSTRACT The present application provides novel tetrahydro – isohumulone ( THIAA ) derivatives and substantially enantiomerically pure compositions and pharmaceutical formulations thereof . The application further provides methods of using the disclosed compounds and compositions to activate PPARy , inhibit inflammation , and treat conditions associated with inflammation and conditions responsive to PPARY modulation such
Comparative Evaluation of Gemcabene and Peroxisome Proliferator–Activated Receptor Ligands in Transcriptional Assays of Peroxisome Proliferator–Activated Receptors: Implication for the Treatment of Hyperlipidemia and Cardiovascular Disease
ABSTRACT Gemcabene, a late-stage clinical candidate, has shown efficacy for LDL-C, non-HDL cholesterol, apoB, triglycerides, and hsCRP reduction, all risk factors for cardiovascular disease. In rodents, gemcabene showed changes in targets, including apoC-III, apoA-I, peroxisomal enzymes, considered regulated through peroxisome proliferator–activated receptor (PPAR) gene activation, suggesting a PPAR-mediated mechanism of action for the observed hypolipidemic effects observed
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
Structural basis for differential activities of enantiomeric PPARγ agonists: Binding of S35 to the alternative site
ABSTRACT Peroxisome proliferator-activated receptor γ (PPARγ) is a member of the nuclear receptor superfamily. It functions as a ligand-activated transcription factor and plays important roles in the regulation of adipocyte differentiation, type 2 diabetes mellitus, and inflammation. Many PPARγ agonists bind to the canonical ligand-binding pocket near the activation function-2 (AF-2) helix (i.e., helix H12)
ABSTRACT Focal adipose deficiency, such as lipoatrophy, lumpectomy or facial trauma, is a formidable challenge in reconstructive medicine, and yet scarcely investigated in experimental studies. Here, we report that Pyrintegrin (Ptn), a 2,4-disubstituted pyrimidine known to promote embryonic stem cells survival, is robustly adipogenic and induces postnatal adipose tissue formation in vivo of transplanted adipose
Lesinurad, a novel, oral compound for gout, acts to decrease serum uric acid through inhibition of urate transporters in the kidney
ABSTRACT Background Excess body burden of uric acid promotes gout. Diminished renal clearance of uric acid causes hyperuricemia in most patients with gout, and the renal urate transporter (URAT)1 is important for regulation of serum uric acid (sUA) levels. The URAT1 inhibitors probenecid and benzbromarone are used as gout therapies; however, their use is limited
Leoligin, the major lignan from edelweiss, inhibits 3-hydroxy-3-methyl-glutaryl-CoA reductase and reduces cholesterol levels in ApoE −/− mice
ABSTRACT The health benefit through the control of lipid levels in hyperlipidaemic individuals is evident from a large number of studies. The pharmacological options to achieve this goal shall be as specific and personalized as the reasons for and co-factors of hyperlipidaemia. It was the goal of this study to reveal the impact of leoligin