Catalog No.
Product Name
Application
Product Information
Citations
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MPC inhibitor
MSDC-0602, a PPARγ-sparing thiazolidinedione (TZD), interacts with the mitochondrial pyruvate carrier (MPC) and inhibits its activity and are effective for treatment of type 2 diabetes with reducing risk of PPARγ-mediated side effects. -
PPARγ modulator
GSK376501A is a selective peroxisome proliferator-activated receptor gamma (PPARγ) modulator for the treatment of type 2 diabetes mellitus. -
PPAR-γ partial agonist
Balaglitazone is a novel partial agonist of PPAR-gamma (γ). -
CYP2C19/CYP2B6 inhibitor
Choline Fenofibrate (ABT-335) is the choline salt of fenofibric acid under clinical development as a combination therapy with rosuvastatin for the management of dyslipidemia. -
PPARγ agonist
Inolitazone dihydrochloride is a novel high-affinity PPARγ agonist, which activates PPARγ with an EC50 about 1/50 that of rosiglitazone and has no effect on RIE cells. -
anti-cancer agent
Falcarindiol (FAD, (3R,8S)-Falcarindiol, FaDOH) is a natural polyacetylene compound found rich in many plants of the Umbelliferae family. Falcarindiol suppresses LPS-stimulated expression of inducible nitric oxide synthase (iNOS), tumor necrosis factor alpha (TNFα), interleukin-6 (IL-6), and interleukin-1 beta (IL-1β). Falcarindiol attenuates the LPS-induced activation of JNK, ERK, STAT1, and STAT3 signaling molecules. Falnidamol is a pyrimido-pyrimidine compound with anti-cancer activity. -
PPAR agonist
Lanifibranor, also known as IVA-337, is a peroxisome proliferator-activated receptors (PPAR) agonist. -
PPAR agonist
Etofylline, also known as BRN-0251760, is a peroxisome proliferator-activated receptor (PPAR) agonist used to treat respiratory and cardiovascular disorders. Etofylline is often used as a bronchodilator. -
penicillin binding protein inhibitor
Cefminox Sodium, also known as Meicelin and MT-141, is a penicillin binding protein inhibitor used to treat bacterial infection. - 6-?Thioinosine (6TI) is a purine antimetabolite, acts as an anti-adipogenesis agent, downregulates mRNA levels of PPAR γ and C/EBPα, as well as PPAR γ target protein such as LPL, CD36, aP2, and LXRα.
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PPARγ Inhibitor
Soyasaponin Ab is a potent PPARγ inhibitor with oral bioavailability. It effectively suppresses PPARγ transcriptional activity and induces apoptosis at elevated concentrations. This compound exhibits a range of biological activities, including anti-obesity, anti-oxidation, anti-inflammation, and anti-aging effects. Additionally, Soyasaponin Ab has been shown to mitigate memory impairment induced by Scopolamine, making it a valuable reagent for research in metabolic and neuroprotective applications. -
PPAR Activator
Rosiglitazone sodium is a potent and selective activator of the peroxisome proliferator-activated receptor gamma (PPARγ), exhibiting EC50 values of 30 nM, 100 nM, and 60 nM for PPARγ1, PPARγ2, and PPARγ, respectively, with a Kd of approximately 40 nM. In addition to its role as a PPARγ activator, Rosiglitazone sodium functions as a modulator of transient receptor potential (TRP) channels, specifically inhibiting TRP melastatin 2 (TRPM2) and TRPM3, while activating TRP canonical 5 (TRPC5). This compound is utilized in research related to metabolic disorders, obesity, and other conditions linked to PPARγ signaling. -
Pan-PPAR Agonist, HIF-1α Inhibitor
Bavachinin is a pan-peroxisome proliferator-activated receptor (PPAR) agonist and a HIF-1α inhibitor, demonstrating IC50 values of 21.043 μM, 12.819 μM, and 0.622 μM for PPAR-α, PPAR-β/δ, and PPAR-γ, respectively. This compound exhibits significant antitumor activity against non-small cell lung cancer through its modulation of PPAR-γ. Additionally, Bavachinin possesses notable anti-inflammatory and anti-angiogenic properties, making it a valuable tool for research in cancer and metabolic disorders. Its oral bioavailability further supports its utility in various biological studies. -
PPARG Inverse Agonist
FX-909 is a covalent inverse agonist of peroxisome proliferator-activated receptor gamma (PPARG), functioning through modulation of receptor activity. This compound exhibits promising biological activity by inhibiting PPARG-mediated signaling pathways, which are often implicated in cancer progression. FX-909 is utilized in cancer research to investigate the effects of PPARG inhibition on tumor growth and survival, providing insights into potential therapeutic targets. -
PPARγ/PPARδ Agonist
15-Deoxy-Δ-12,14-prostaglandin J2 (15d-PGJ2) is an endogenous cyclopentenone prostaglandin that targets peroxisome proliferator-activated receptors, specifically acting as a selective agonist for PPARγ with an EC50 of 2 µM and a covalent agonist for PPARδ. This compound is known to facilitate the differentiation of C3H10T1/2 fibroblasts into adipocytes with an EC50 of 7 μM. Due to its effects on adipogenesis and metabolism, 15d-PGJ2 is utilized in research exploring obesity, diabetes, and metabolic syndrome pathways. -
PPARδ Agonist
Seladelpar sodium salt is a potent and selective agonist of the PPARδ receptor, demonstrating an EC50 of 2 nM. It exhibits more than 750-fold selectivity over PPARα and 2500-fold selectivity over PPARγ. This compound is primarily utilized in research regarding primary biliary cholangitis, contributing to the understanding of metabolic and inflammatory pathways. -
PPARγ Antagonist
SR1664 is a potent antagonist of peroxisome proliferator-activated receptor gamma (PPARγ). It effectively binds to PPARγ and inhibits Cdk5-mediated phosphorylation of the receptor, demonstrating an IC50 value of 80 nM and a Ki of 28.67 nM. This compound has valuable applications in research focused on metabolic regulation and the development of therapeutic strategies for conditions such as obesity and diabetes. -
PPARγ Activator
Convallatoxin is a PPARγ activator derived from the plant Adonis amurensis. It exhibits significant anti-inflammatory effects by mitigating colitic inflammation through the activation of PPARγ and the suppression of NF-κB signaling pathways. Additionally, Convallatoxin serves as a substrate for P-glycoprotein, identifying Val982 as a critical amino acid for its transport. This compound also enhances ligand-induced micro-opioid receptor (MOR) endocytosis, demonstrating high potency and efficacy, making it valuable for research in inflammation and cellular signaling. -
PPAR-γ Activator
Glabrone, a PPAR-γ activator derived from the roots of Glycyrrhiza glabra, demonstrates notable ligand binding activity to this nuclear receptor. In addition to its role as a specific probe substrate for UGT1A9, Glabrone's metabolites inhibit neuraminidase, thus preventing influenza virus release. This compound is suitable for research applications focused on herb-drug interactions and the evaluation of anti-influenza viral activity. -
PPARγ Activator/Mitochondrial Dysfunction Inducer
(S)-Coriolic acid is a potent PPARγ activator formed through the metabolism of linoleic acid by 15-lipoxygenase (15-LOX). This compound serves as a crucial intracellular signaling agent, influencing cell proliferation and differentiation across diverse biological systems. Additionally, (S)-Coriolic acid is known to induce mitochondrial dysfunction and contribute to airway epithelial injury, making it relevant for studies investigating cellular stress responses and respiratory health. -
PPARγ Inhibitor
PPARγ-IN-2 is a selective PPARγ inhibitor that effectively reduces triglyceride accumulation in 3T3-L1 preadipocytes, with an EC50 of 0.106 μM. This compound demonstrates potential for mitigating obesity and associated metabolic syndrome, particularly in the context of a high-cholesterol diet. Its ability to diminish lipid accumulation in adipose tissue makes it a valuable tool for research focused on metabolic disorders and adipocyte biology. -
PPARγ Activator
SDPC (DHA-PC) is a PPARγ activator that demonstrates significant anti-angiogenic properties. This phospholipid, featuring an ester bond with docosahexaenoic acid (DHA) at the sn-2 position, effectively inhibits the proliferation, migration, and tube formation of human umbilical vein endothelial cells. SDPC holds potential for applications in anti-tumor angiogenesis research, making it a valuable tool for studying tumor progression and vascular growth inhibition. -
PPARγ Agonist
AMG131 is a selective peroxisome proliferator-activated receptor γ (PPARγ) modulator, functioning as a potent non-thiazolidinedione (TZD) agonist. It binds to PPARγ in the same pocket as TZDs, yet interacts with the receptor at unique contact points, potentially leading to differential biological effects. This compound has significant potential for research applications related to type-2 diabetes mellitus and metabolic disorders. -
PPAR-δ Modulator
Bocidelpar is a selective PPAR-δ modulator that activates the PPAR-δ downstream signaling pathway, leading to the upregulation of target genes such as ABCA1 and ACAA2. This compound promotes fatty acid oxidation and enhances mitochondrial biogenesis, ultimately improving mitochondrial dysfunction. Bocidelpar is particularly useful in researching diseases associated with mitochondrial dysfunction, including primary mitochondrial myopathy (PMM) and Duchenne muscular dystrophy (DMD). -
PPARγ Antagonist
Mifobate is a potent antagonist of peroxisome proliferator-activated receptor gamma (PPARγ), selectively inhibiting thiazolidinedione (TZD)-induced transcriptional activity with an IC50 of 140 μM. This compound does not affect the basal or ligand-stimulated transcriptional activity of PPARα, PPARβ, or the farnesoid X receptor (FXR). Mifobate demonstrates significant antiobesity and antidiabetic effects, making it valuable for research applications aimed at exploring metabolic disorders and therapeutic interventions for related conditions. -
PPARγ Agonist
Leriglitazone hydrochloride is a potent agonist of the peroxisome proliferator-activated receptor gamma (PPARγ), with an EC50 of 9 μM. This compound is orally active and capable of penetrating the blood-brain barrier, exhibiting neuroprotective, anti-inflammatory, and antioxidant properties. Leriglitazone hydrochloride is suitable for research focused on neuroinflammatory and neurodegenerative diseases, providing valuable insights into mitochondrial function regulation. -
PPAR Agonist
Raspberry ketone is a potent PPAR-α agonist known for its role in lipid metabolism regulation. This naturally occurring aromatic compound, primarily derived from red raspberries, exhibits significant biological activity that may contribute to weight management and metabolic health research. Its applications extend to studying the effects on obesity and diabetes through modulation of lipid profiles and glucose homeostasis. -
PPAR Agonist
4-O-Methyl honokiol is a natural neolignan derived from Magnolia officinalis that functions as a selective PPARγ agonist. It exhibits significant inhibition of NF-κB activity, making it a valuable tool for studying mechanisms of inflammation and cancer. Its biological activity is particularly relevant in research focused on metabolic regulation and inflammatory responses. -
PPARγ inhibitor
SR 16832 is a dual-site covalent inhibitor of peroxisome proliferator-activated receptor gamma (PPARγ). It functions by targeting both orthosteric and allosteric sites, leading to significant modulation of PPARγ activity. This compound is valuable for research applications related to metabolic disorders, obesity, and diabetes, particularly in studies investigating the downstream effects of PPARγ inhibition on gene expression and cellular metabolism. -
PPAR-γ Agonist
Darglitazone is a thiazolidinedione and a potent, selective agonist of peroxisome proliferator-activated receptor gamma (PPAR-γ). It plays a significant role in the regulation of glucose homeostasis and lipid metabolism. Darglitazone is utilized in research focused on type II diabetes and related metabolic disorders, providing insights into its effects on insulin sensitivity and adipogenesis. -
PPARα Agonist
10-Hydroxystearic acid (10-HSA) is a PPARα agonist that promotes collagen synthesis. This compound exhibits significant anti-aging properties by enhancing skin texture, reducing the appearance of pores, and diminishing hyperpigmented lesions. 10-HSA is valuable for research focused on skin health, regenerative medicine, and dermatological studies. -
PPARα Activator
(10E,12Z)-Octadeca-10,12-dienoic acid is a potent PPARα activator that plays a critical role in regulating lipid metabolism and adipocyte differentiation. This compound has demonstrated various biological activities, including antioxidant and antitumor effects, alongside the induction of proinflammatory cytokines and chemokines, which may contribute to decreased adipogenesis and insulin resistance. (10E,12Z)-Octadeca-10,12-dienoic acid also influences milk fat synthesis by reducing the expression of lipogenic enzymes and inhibiting fatty acid desaturation. Additionally, it has been shown to modulate lipoprotein lipase activity in cultured adipocytes and alter hepatic stearoyl-CoA desaturase expression in vivo. -
PPARG Inhibitor
FTX-6746 is an orally active inhibitor of peroxisome proliferator-activated receptor gamma (PPARG). It demonstrates significant tumor inhibition in mouse xenograft models, making it a valuable tool for investigating the therapeutic potential of targeting PPARG in cancer research. Its specificity and efficacy in modulating PPARG activity support its use in studies related to metabolic disorders and cancer biology. -
PPARγ Inverse-Agonist
BAY-4931 is a selective inverse agonist of PPARγ, exhibiting potent action with an IC50 of 0.17 nM. This compound effectively modulates PPARγ activity, making it a valuable tool for investigating metabolic disorders and insulin sensitivity. Its unique mechanism of action allows for detailed studies of PPARγ's role in various biological processes and therapeutic applications. -
PPARβ/δ Inverse Agonist
ST247 is a potent inverse agonist of the peroxisome proliferator-activated receptor beta/delta (PPARβ/δ). It exhibits a high affinity for this target and modulates the expression of the activation marker CCL2 in a manner contrary to typical agonist activity. ST247 effectively promotes the interaction with corepressors and inhibits agonist-induced transcriptional activity of PPARβ/δ. This compound is valuable for research into metabolic disorders and inflammation, offering insights into the regulatory mechanisms mediated by PPARβ/δ. -
PPARγ Agonist
Edaglitazone is a selective and orally bioactive agonist of PPARγ, exhibiting an EC50 of 1053 nM for this target, alongside a lower affinity for PPARα at 35.6 nM. This compound demonstrates significant antidiabetic and anti-hyperglycemic properties, making it a valuable tool in diabetes research. Its ability to modulate metabolic pathways underscores its potential applications in studies related to glucose homeostasis and cardiovascular health. -
PPARα/γ Agonist
Saroglitazar magnesium is a selective agonist of peroxisome proliferator-activated receptors PPARα and PPARγ, exhibiting high potency with EC50 values of 0.65 pM and 3 nM, respectively, in HepG2 cells. This compound plays a crucial role in lipid metabolism and glucose homeostasis, making it a valuable tool for research in metabolic disorders such as dyslipidemia and type 2 diabetes. Its dual activity on PPARα and PPARγ positions it as a significant candidate for exploring therapeutic strategies in metabolic disease models. -
PPARδ Agonist
Mavodelpar is a selective PPARδ agonist that exerts protective effects against glomerular injury and renal fibrosis. This compound is particularly relevant in research focused on primary mitochondrial myopathies (PMM) and long-chain fatty acid oxidation disorders (LC-FAOD). Additionally, Mavodelpar features an alkyne functional group, enabling it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc) for click chemistry applications. -
PPARα Agonist
GW 590735 is a potent and selective PPARα agonist, exhibiting an EC50 of 4 nM with over 500-fold selectivity for PPARα compared to PPARδ and PPARγ. This compound is valuable for research focused on dyslipidemia and metabolic disorders, facilitating insights into lipid metabolism and potential therapeutic approaches targeting PPARα. -
PPAR Antagonist
H-Trp-Glu-OH is a selective and reversible antagonist of peroxisome proliferator-activated receptor gamma (PPARγ), with a dissociation constant (Kd) of approximately 8 µM. This compound has demonstrated cell permeability and presents potential as a lead compound in diabetes research. Its role in modulating PPARγ activity makes it an important tool for studying metabolic disorders and associated therapeutic pathways. -
PPARα Agonist
GW 9578 is a selective agonist of the peroxisome proliferator-activated receptor alpha (PPARα), exhibiting EC50 values of 5 nM for murine PPARα and 50 nM for human PPARα. This compound demonstrates significant lipid-lowering activity, making it a valuable tool for research in metabolic disorders and cardiovascular diseases. GW 9578 may be utilized in studies investigating the role of PPARα activation in lipid metabolism and related therapeutic applications. -
PPARγ Agonist
FK614 is a selective PPARγ modulator (SPPARM) that functions as a PPARγ agonist with significant anti-diabetic properties. This compound exhibits distinct effects on PPARγ activation throughout various stages of adipocyte differentiation. FK614 is utilized in research focused on hyperglycemia, hypertriglyceridemia, glucose intolerance, and type 2 diabetes, making it a valuable tool for understanding metabolic disorders. -
PPARα/PPARγ Inhibitor
Netoglitazone is a dual agonist targeting PPARα and PPARγ, exhibiting significant antihyperglycemic activity. This compound is instrumental in metabolic research and provides insights into the regulation of glucose homeostasis. Its application in studies related to diabetes and metabolic syndrome makes it a valuable tool for exploring therapeutic strategies. -
PPAR Activator
2-(Tetradecylthio)acetic acid is a pan-peroxisome proliferator-activated receptor (pan-PPAR) activator. This compound is known to induce hypolipidemia by reducing plasma lipid levels and enhancing hepatic fatty acid oxidation in rodent models. Additionally, it increases the expression of genes associated with fatty acid uptake, activation, accumulation, and oxidation, making it a valuable tool for research on lipid metabolism and related disorders. -
PPARγ agonist
Rivoglitazone is a thiazolidinedione derivative that functions as a selective PPARγ agonist. This compound is primarily used in research focused on the pathophysiology of type 2 diabetes mellitus and the regulation of glucose metabolism. Its activation of PPARγ has implications for insulin sensitivity and adipocyte function, making it a valuable tool in diabetes research and drug discovery. -
PPARγ Inhibitor
trans-Cinnamyl alcohol is a selective PPARγ inhibitor that plays a significant role in regulating lipid metabolism and adipogenesis. As a metabolite derived from chestnut flowers, it exhibits anti-obesity activity by inhibiting PPARγ expression. This compound is valuable for research applications focused on obesity, metabolic disorders, and the modulation of fat cell differentiation. -
PPARG Inverse-agonist
BAY-5516 is an inverse agonist of PPARG, exhibiting an IC50 value of 6.1 ± 3.6 nM. This compound demonstrates significant anti-tumor activity, making it a valuable tool for research into cancer therapeutics. It is suitable for studies focusing on the modulation of PPARG signaling pathways and their implications in various tumor models. -
PPAR Activator
8(S)-HETE (8(S)-Hydroxyeicosatetraenoic acid) primarily acts as a PPARα activator, with demonstrated biological activity in stimulating mouse keratinocyte protein kinase C at an IC50 of 100 μM. This compound selectively activates PPARα at concentrations as low as 0.3 μM, making it valuable for research into skin biology and inflammatory responses. The stereochemical assignment of the (S) enantiomer is confirmed through chiral HPLC retention time comparisons with established data.
