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  • HOME
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    • About
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    • Ortholog Assays
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    • In Vitro Toxicology Platform
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    • Gene Expression
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    • Live Cell Multiplex
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Peroxisome Proliferator-Activated Receptor Gamma (PPARγ; NR1C3)

Product Family Product Number Product Description Technical Manual
IB0010
PPARγ
(NR1C3)
IB00101-32 Human PPARγ Reporter Assay System, 3 x 32 assays in 96-well format Technical Manual
IB00101 Human PPARγ Reporter Assay System, 1 x 96-well format assays Technical Manual
IB00102 Human PPARγ Reporter Assay System, 1 x 384-well format assays Technical Manual
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Also available in: Mouse/Rat Shared Ortholog, Cyn Monkey, Zebrafish

This Peroxisome Proliferator-Activated Receptor Gamma (PPARγ) kit is an all-inclusive assay system that includes, in addition to PPARγ 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.

PPARγ 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 PPARγ 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.

Kits are offered in different assay formats to accommodate researchers’ needs: 3x 32, 1x 96, and 1x 384 assay formats for screening small numbers of test compounds, as well as custom bulk reagents for HTS applications.

Human Peroxisome Proliferator-Activated Receptor Gamma agagonistHuman Peroxisome Proliferator-Activated Receptor Gamma antagonist

Assay Kit & Platforms

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

Also available in: Mouse/Rat Shared Ortholog, Cyn Monkey. Zebrafish

Peroxisome Proliferator-Activated Receptor Gamma (PPARγ), also known as the glitazone receptor, or NR1C3 is a type II nuclear receptor that in humans is encoded by the PPARγ 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 PPARγ Reporter Assay System utilize proprietary mammalian cells engineered to express human PPARG, commonly referred to as PPARγ.

The principle application of this assay product is in the screening of test samples to quantify functional activities, either agonist or antagonist, that they may exert against the human peroxisome proliferator-activated receptor gamma.

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

Service Assays: Human, Rat/Mouse Shared Ortholog, Cyn Monkey, 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.

Diabetes; Obesity; Cancer; Inflammation; Lipid Metabolism and Energy; Metabolic Disease; NAFLD/NASH; Environmental Toxicology

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 mostRead More

Posted in New Publications | Tagged PPARg, PPARγ | Comments Off on Lipoxygenase catalyzed metabolites derived from docosahexaenoic acid are promising antitumor agents against breast cancer

Nuclear Receptors Regulate Intestinal Inflammation in the Context of IBD

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 underlyingRead More

Posted in New Publications | Tagged glucocorticoids, GR, ibd, Inflammation, intestinal inflammation, nuclear receptors, PPARγ, PXR, VDR | Comments Off on Nuclear Receptors Regulate Intestinal Inflammation in the Context of IBD

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 heatedRead More

Posted in New Publications | Tagged Carnosic acid, carnosol, PPAR gamma, PPARγ | Comments Off on Structures and biological activities of new carnosic acid- and carnosol-related compounds generated by heat treatment of rosemary

Tetrahydro-Isohumulone Derivatives, Methods of Making and Using: Patent Application

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 suchRead More

Posted in New Publications | Tagged patent, PPAR, PPARγ | Comments Off on Tetrahydro-Isohumulone Derivatives, Methods of Making and Using: Patent Application

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 observedRead More

Posted in New Publications | Tagged gemcabene, nuclear hormone receptors, PPARα, PPARγ, PPARδ, transactivation | Comments Off on 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

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 partialRead More

Posted in New Publications | Tagged glucose metabolism, glucose stimulated insulin secretion, ortholog, PPAR, PPARα, PPARβ, PPARγ, rat PPAR | Comments Off on GPR40 partial agonist MK-2305 lower fasting glucose in the Goto Kakizaki rat via suppression of endogenous glucose production

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)Read More

Posted in New Publications | Tagged enantiomeric PPARγ, PPAR, PPARγ, PPARγ agonist | Comments Off on Structural basis for differential activities of enantiomeric PPARγ agonists: Binding of S35 to the alternative site

Pyrintegrin Induces Soft Tissue Formation by Transplanted or Endogenous Cells

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 adiposeRead More

Posted in New Publications | Tagged PPAR, PPARγ | Comments Off on Pyrintegrin Induces Soft Tissue Formation by Transplanted or Endogenous Cells

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 limitedRead More

Posted in New Publications | Tagged PPAR, PPARγ | Comments Off on Lesinurad, a novel, oral compound for gout, acts to decrease serum uric acid through inhibition of urate transporters in the kidney

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 leoliginRead More

Posted in New Publications | Tagged ortholog, PPAR, PPARγ | Comments Off on Leoligin, the major lignan from edelweiss, inhibits 3-hydroxy-3-methyl-glutaryl-CoA reductase and reduces cholesterol levels in ApoE −/− mice
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