Catalog No.
Product Name
Application
Product Information
Citations
-
PPARγ Agonist
Caulophyllogenin is a triterpene saponin that acts as a partial agonist of PPARγ, exhibiting an EC50 of 12.6 μM. This compound plays a significant role in the modulation of glucose metabolism and adipogenesis, making it relevant for research on type-2 diabetes, obesity, metabolic syndrome, and inflammation. Its distinct biological activity allows for further exploration in the development of therapeutic strategies targeting metabolic disorders. -
PPAR-γ Modulator
PA-082 is a selective modulator of peroxisome proliferator-activated receptor gamma (PPAR-γ) functioning as a partial agonist. It promotes the partial recruitment of coactivators SRC1, TIF2, and SRC3, while fully recruiting PGC1-α to the PPAR-γ ligand-binding domain. PA-082 effectively inhibits triglyceride accumulation during de novo adipogenesis and counteracts lipid buildup induced by Rosiglitazone. Furthermore, this compound enhances insulin-stimulated glucose uptake in adipocytes and provides protection against TNFα-induced insulin resistance, making it a valuable tool for research into type 2 diabetes. -
PPAR Activator
NC-2100 is a selective peroxisome proliferator-activated receptor (PPAR) activator. It has demonstrated efficacy in reducing plasma glucose and triglyceride levels in obese KKAy mice, making it a valuable tool for studying metabolic disorders. Additionally, NC-2100 induces the expression of uncoupling proteins UCP1 and UCP2 in mesenteric and subcutaneous white adipose tissue. This compound is suitable for research applications related to type 2 diabetes and metabolic regulation. -
PPAR Agonist
Sodelglitazar is a pan-PPAR agonist that targets peroxisome proliferator-activated receptors (PPARs), which play a crucial role in lipid metabolism and glucose homeostasis. This compound exhibits significant biological activity in regulating lipid profiles and enhancing insulin sensitivity, making it a promising candidate for the treatment of hyperlipidemia and type 2 diabetes. Research applications include studies focused on metabolic disorders and the exploration of PPAR signaling pathways. -
PPARγ/TRPA1 Receptor Partial Agonist
Neoambrosin is a sesquiterpene lactone that acts as a partial agonist of the PPARγ and TRPA1 receptors. This compound demonstrates potential biological activity related to hypoglycemia, analgesia, anti-inflammatory responses, and anticancer effects. Neoambrosin is suitable for research applications aimed at exploring metabolic disorders and pain management, as well as studying its role in inflammation and cancer therapeutics. -
PPAR Agonist
20-HEPE is a metabolite of eicosapentaenoic acid that functions primarily as a peroxisome proliferator-activated receptor α (PPARα) agonist. At a concentration of 10 μM, it effectively activates PPARα in COS-7 cells that express a luciferase reporter gene. Additionally, 20-HEPE activates the mouse transient receptor potential vanilloid receptor 1 (mTRPV1) in vitro, although it does not exhibit analgesic effects in rat models. This compound has potential applications in the study of metabolic processes and receptor signaling pathways. -
PPARβ/δ Antagonist
CC618 is a selective antagonist of the peroxisome proliferator-activated receptor beta/delta (PPARβ/δ). This compound exhibits its antagonistic effects by covalently binding to PPARβ/δ receptors, modulating their activity. As a result, CC618 is valuable for exploring the roles of PPARβ/δ in various biological processes and disease states, making it a useful tool in metabolic research and studies related to inflammation and cancer. -
PPAR-γ Agonist
Darglitazone Sodium is a potent and selective agonist of the peroxisome proliferator-activated receptor-gamma (PPAR-γ), belonging to the thiazolidinedione class of compounds. It plays a crucial role in regulating blood glucose levels and lipid metabolism, making it valuable for research focused on type II diabetes and related metabolic disorders. This compound offers an effective tool for investigating the mechanisms underlying insulin sensitivity and adipocyte differentiation. -
PPAR Activator
Ronifibrate is a fibrate that acts as a PPARα activator, effectively modulating lipid metabolism. It is primarily utilized in research focused on hyperlipidemia and the associated metabolic disorders. By activating PPARα, Ronifibrate influences fatty acid oxidation and lipoprotein metabolism, making it a valuable tool for studying dyslipidemia and cardiovascular risks. -
PPARγ Agonist
PPARγ agonist 3 is a selective agonist of the peroxisome proliferator-activated receptor gamma (PPARγ), playing a crucial role in regulating glucose metabolism and adipogenesis. This compound is characterized by its strong biological activity, demonstrating the ability to enhance antitumor efficacy when used in conjunction with Imatinib. Importantly, PPARγ agonist 3 exhibits low cytotoxicity in both resistant and non-resistant cell lines, making it a valuable tool for cancer research and metabolic studies. -
PPAR Agonist
Rac-Pemafibrate is a potent PPARα agonist, effectively activating PPARα with an EC50 of 1 nM, while also showing activity for PPARγ and PPARδ with EC50 values exceeding 10 μM and 1.7 μM, respectively. This racemic compound is essential for research focused on metabolic disorders, lipid metabolism, and inflammation, providing insights into the role of PPARs in these biological pathways. It serves as a valuable tool for studying PPAR-related mechanisms and therapeutic interventions. -
PPAR Modulator
PPARγ/δ modulator 1 is a selective modulator of the peroxisome proliferator-activated receptors (PPARs), acting as an antagonist for PPARδ and a partial agonist for PPARγ. It exhibits Ki values of 14.4 nM for PPARδ and 5.31 μM for PPARγ, indicating strong binding affinity. This compound demonstrates biological activities with an EC50 of 7.3 μM for PPARδ corepression and 12.6 μM for the stimulation of adiponectin production. Its modulation capabilities make it a valuable tool for research on metabolic disorders and related pathways. -
PPARα Agonist
ESP-31015 is an orally active agonist of PPARα, a key regulator of lipid metabolism. It exhibits significant lipid-regulating effects demonstrated in the obese Zucker rat model, making it a valuable tool for studying dyslipidemia. This compound is applicable in cardiovascular disease research, offering insights into mechanisms of metabolic regulation and potential therapeutic strategies. -
PPAR Agonist
GSK-7227 is a partial agonist of the peroxisome proliferator-activated receptor delta (PPARδ). It effectively regulates the expression of target genes associated with lipid metabolism, specifically CPT1a and PDK4, in skeletal muscle cells. This compound holds potential for studies focused on metabolic disorders and mitochondrial function modulation. -
PPARγ Agonist
S26948 is a high-affinity agonist of peroxisome proliferator-activated receptor γ (PPARγ), demonstrating an EC50 of 8.83 nM. This compound exhibits significant antidiabetic and antiatherogenic properties, making it a valuable tool for research in metabolic disorders. It can be utilized to investigate the mechanisms underlying insulin sensitivity and lipid metabolism. -
PPARγ Agonist
GW1929 hydrochloride is a potent agonist of the peroxisome proliferator-activated receptor-γ (PPARγ), exhibiting a pKi of 8.84 for human PPAR-γ and pEC50 values of 8.56 for human PPAR-γ and 8.27 for murine PPAR-γ. This compound demonstrates significant antidiabetic activity and potential neuroprotective effects by suppressing neuronal apoptosis and exhibiting anti-inflammatory properties. It is a valuable tool for investigating metabolic disorders, neurodegenerative diseases, and the mechanisms of inflammation in research applications. -
PPARγ Partial Agonist
GSK 1997132B is a benzimidazole-derived partial agonist of PPARγ, notable for its ability to cross the blood-brain barrier with a pEC50 value of 8.0. This compound selectively activates PPARγ while exhibiting minimal activity on PPARα and PPARδ, addressing issues related to high blood clearance rates seen in earlier agents. GSK 1997132B is particularly relevant for research into Alzheimer's disease, providing a potential pathway for exploring therapeutic strategies that mitigate associated side effects such as weight gain and edema. -
PPARα Agonist
AZD4619 is a selective agonist of the peroxisome proliferator-activated receptor α (PPARα) with oral bioactivity. It has been demonstrated to enhance the expression of alanine aminotransferase 1 (ALT1) protein in a dose-dependent manner in human primary hepatocytes, though this effect is not observed in rat hepatocytes. This compound is primarily utilized in research related to lipid metabolism and is of interest in the development of lipid-lowering therapeutics. -
PPARγ Agonist
PPARγ Agonist 6 is a potent and selective agonist of peroxisome proliferator-activated receptor gamma (PPARγ). This compound enhances PPARγ-mediated transcriptional activity, influencing insulin sensitivity and adipogenesis. It is valuable for investigating the role of PPARγ in cancer biology and metabolic disorders. -
PPAR Agonist
Nor-LY-510929 is a selective agonist of the peroxisome proliferator-activated receptor (PPAR), primarily involved in the regulation of lipid metabolism and glucose homeostasis. This compound exhibits potent biological activity in modulating PPAR signaling pathways, making it useful for researching metabolic disorders and related endocrine functions. Its application may provide insights into therapeutic strategies for conditions such as obesity, type 2 diabetes, and dyslipidemia. -
PPAR-γ Agonist
Rivoglitazone hydrochloride is a potent peroxisome proliferator-activated receptor-γ (PPAR-γ) agonist. By activating PPAR-γ, it modulates the expression of genes involved in lipid and glucose metabolism, thereby exerting significant anti-diabetic effects. This compound is valuable for research applications focusing on insulin secretion and insulin resistance, particularly in animal models of diabetes. -
PPARα/γ Agonist
MD001 is a dual agonist of PPARα and PPARγ, targeting both receptors to enhance their transcriptional activity. This compound promotes the expression of genes associated with β-oxidation, as well as fatty acid and glucose uptake, making it a valuable tool for research in metabolic disorders and insulin sensitivity. MD001 holds potential in exploring therapeutic strategies for conditions such as obesity and type 2 diabetes. -
PPARG Inverse Agonist
BAY-9683 is an orally active covalent inverse agonist of PPARG (Peroxisome Proliferator-Activated Receptor Gamma). It effectively inhibits the activity of overactive PPARG, making it a valuable tool for investigating diseases associated with PPARG dysregulation, including luminal bladder cancer. This compound is suitable for research applications focused on metabolic regulation and cancer biology. -
PPARγ Agonist
(R)-Pioglitazone is a selective agonist of the peroxisome proliferator-activated receptor gamma (PPARγ), exhibiting high affinity for the PPARγ ligand-binding domain. This R enantiomer is shown to be orally active, making it a valuable tool in the investigation of metabolic regulation. Its potential applications extend to research in neurodegenerative diseases, particularly Alzheimer's disease, where modulation of PPARγ pathways may influence disease progression and pathology. -
PPARg Ligand
L-764406 is a high-affinity non-thiazolidinedione ligand for the peroxisome proliferator-activated receptor gamma (PPARγ). Demonstrating partial agonist activity, L-764406 activates the expression of adipocyte-specific genes, such as aP2, in both chimeric receptors containing the PPARγ ligand-binding domain and in 3T3-L1 cell models. Notably, L-764406 does not exhibit activity with PPARα or PPARδ, making it a selective tool for studying PPARγ-related pathways and their implications in metabolic research. -
PPARγ Agonist
PPARγ Agonist 1 is a selective agonist of the peroxisome proliferator-activated receptor gamma (PPARγ). This compound effectively activates human PPARγ, functioning as a partial agonist, which may help circumvent adverse effects commonly associated with full agonism. PPARγ Agonist 1 is particularly relevant for research in cardiovascular diseases linked to metabolic disorders, providing insights into therapeutic strategies targeting metabolic regulation and cardiovascular health. -
PPARγ Agonist
Cinoxate is a selective agonist of peroxisome proliferator-activated receptor gamma (PPARγ), exhibiting a Ki value of 18.0 μM. This compound is utilized in research to investigate metabolic disorders, particularly obesity, by modulating adipocyte differentiation and lipid metabolism. Its activation of PPARγ may also provide insights into associated pathways, aiding in the understanding of insulin sensitivity and energy homeostasis. -
PPARα/PPARγ Agonist
Cevoglitazar is a potent dual agonist of PPARα and PPARγ, designed for oral administration. It effectively reduces food intake, body weight, and fasting plasma insulin levels in preclinical models such as obese mice and cynomolgus monkeys. This compound holds promise for research into diabetes and obesity-related disorders, facilitating exploration of metabolic pathways and therapeutic strategies in these conditions. -
PPAR/ sEH Modulator
SP-C01 is a potent modulator targeting soluble epoxide hydrolase (sEH) and serving as a partial agonist of peroxisome proliferator-activated receptor gamma (PPARγ). This compound exhibits significant inhibitory effects on Ser273 phosphorylation, highlighting its potential role in metabolic research and the modulation of inflammatory pathways. SP-C01 is suitable for studies investigating the therapeutic effects on metabolic disorders and the regulation of lipid metabolism. -
PPARγ Agonist
BR101549 is a non-thiazolidinedione (non-TZD) agonist of peroxisome proliferator-activated receptor gamma (PPARγ). It demonstrates activation of PPARγ comparable to that of Pioglitazone in vitro. This compound has been shown to effectively regulate blood glucose levels in mouse models, making it a valuable tool for anti-diabetic research and studies related to metabolic disorders. -
PPARγ Agonist
PPARγ Agonist 16 acts as a selective agonist for peroxisome proliferator-activated receptor gamma (PPARγ), demonstrating competitive binding to the ligand-binding domain (LBD) with an IC50 of 1790 nM. This compound is notable for its ability to inhibit ear swelling in murine models and shows promising anti-hyperglycemic effects in streptozotocin-induced diabetes models. PPARγ Agonist 16 is valuable for research applications focused on metabolic disorders and inflammation. -
PPAR-γ Activator
Apo-12'-lycopenal is a metabolite of Lycopene acting as a PPAR-γ activator. It is known to enhance adipocyte differentiation and stimulate adiponectin secretion, making it of interest in studies related to metabolic regulation and obesity research. Its role in modulating PPAR-γ activity positions it as a valuable tool for investigating lipid metabolism and insulin sensitivity. -
PPARγ Agonist
AMG131 benzenesulfonate is a selective peroxisome proliferator-activated receptor γ (PPARγ) agonist, classified as a non-thiazolidinedione (TZD) modulator. It binds to the PPARγ receptor, occupying a unique position in the binding pocket, which allows for distinct interactions compared to traditional TZDs. This compound has demonstrated potential in research pertaining to the treatment of type-2 diabetes mellitus, making it a valuable tool for investigating PPARγ-related metabolic pathways. -
PPARγ Agonist
PPARγ agonist 8 is a selective agonist of the peroxisome proliferator-activated receptor gamma (PPARγ). It effectively induces peroxisome proliferator response element (PPRE)-luciferase activity with an EC50 of 0.2 μM, highlighting its potency in modulating PPARγ signaling pathways. This compound is valuable for studying the role of PPARγ in metabolic regulation, insulin sensitivity, and inflammation-related research. -
PPARγ Agonist
DS-6930 is a potent and selective agonist of PPARγ, exhibiting an EC50 of 41 nM. This compound significantly reduces plasma glucose levels while exhibiting fewer PPARγ-related adverse effects compared to traditional agents. DS-6930 is utilized for research in diabetes and metabolic disorders, making it a valuable tool for exploring therapeutic strategies in these areas. -
PPAR Agonist
Reglitazar is a selective agonist for peroxisome proliferator-activated receptors α and β (PPAR α and PPAR β). It is known to enhance insulin sensitivity, reduce blood glucose levels, and regulate lipid metabolism. This compound is useful in research applications focused on metabolic disorders, diabetes, and cardiovascular diseases, providing insights into the modulation of metabolic pathways. -
PPAR Agonist
MHY 553 is a PPARα agonist that enhances fatty acid oxidation and reduces liver fat accumulation. This compound has demonstrated efficacy in mitigating triglyceride accumulation induced by liver X receptor agonists in HepG2 cells. Additionally, MHY 553 significantly suppresses inflammatory mRNA expression in aging rats, making it a valuable tool for research on metabolic disorders and age-related inflammation. -
PPARα/γ Activator
GW-9820 is a potent activator of both PPARα and PPARγ, exhibiting EC50 values of 0.37 μM and 0.288 μM, respectively. This compound has been shown to enhance the expression of CLA-1, a key player in lipid metabolism and inflammation. GW-9820 is primarily utilized in research focused on atherosclerosis, offering insights into the modulation of metabolic pathways linked to cardiovascular diseases. -
PPARα Agonist
KRP-105 is a selective agonist of peroxisome proliferator-activated receptor alpha (PPARα), exhibiting an effective concentration (EC50) of 8 nM. This compound has demonstrated the ability to significantly lower serum levels of triglycerides, total cholesterol, and non-high-density lipoprotein cholesterol. KRP-105 is suitable for research applications focused on metabolic diseases, particularly dyslipidemia. -
PPAR Modulator
SR2595 is an inverse agonist of peroxisome proliferator-activated receptor gamma (PPARγ), exhibiting an IC50 value of 30 nM. This compound functions by modulating PPARγ activity, leading to alterations in gene expression associated with lipid metabolism and insulin sensitivity. SR2595 is primarily used in research related to metabolic disorders, obesity, and diabetes, making it a valuable tool for studying PPARγ signaling pathways and their implications in various physiological processes. -
PPARγ ligand
SR 1824 is a non-agonist ligand for peroxisome proliferator-activated receptor gamma (PPARγ), functioning primarily by inhibiting Cdk5-mediated phosphorylation. This compound exhibits anti-diabetic properties, making it a valuable tool for research focused on metabolic disorders and the modulation of PPARγ signaling pathways. Its unique mechanism supports investigations into the regulation of insulin sensitivity and the therapeutic potential in diabetes-related studies. -
COX-2 Inhibitor/PPAR-γ Activator
Zaltoprofen sulfoxide is a selective COX-2 inhibitor with an IC50 of 45.38 nM, as well as a PPAR-γ activator. This compound effectively inhibits NF-κB and MAPK inflammatory signaling pathways, making it a valuable tool in the study of inflammation and acute lung injury models. It is particularly relevant for research focused on LPS-induced acute lung injury. -
LTD4 Antagonist/PPAR-γ Agonist
LTD4 antagonist 3 (FK011 hydrochloride) is a selective leukotriene D4 (LTD4) antagonist that also exhibits agonistic activity for peroxisome proliferator-activated receptor gamma (PPAR-γ). This compound demonstrates enhanced PPAR-γ activation with a fold-increase of 1.50 at 1 μM and 2.35 at 10 μM. LTD4 antagonist 3 is valuable for research in the development of non-steroidal anti-inflammatory drugs (NSAIDs) and related therapeutic applications targeting inflammatory pathways. -
PPAR Modulator
C333H is a selective modulator of PPARγ, effectively exhibiting insulin-sensitizing and hypoglycemic properties. In diabetic mouse models, C333H demonstrates insulin-sensitizing effects comparable to thiazolidinediones without causing significant weight gain or increased adipose tissue mass. The compound elevates levels of high molecular weight adiponectin isoforms in diabetic db/db mice and reduces serine phosphorylation of PPARγ at residue 273 in brown adipose tissue, selectively modulating the expression of specific target genes in adipose tissue. Additionally, C333H shows weak recruitment of co-activators and weak dissociation of co-repressors in vitro, indicating its potential as an inhibitor of type 2 diabetes. -
PPARδ Agonist
PPARδ Agonist 10 is a selective, orally active partial agonist targeting peroxisome proliferator-activated receptor delta (PPARδ) with EC50 values of 0.053 μM for human PPARδ (LBD) and 0.30 μM for mouse PPARδ. This compound exhibits full agonistic activity on free fatty acid oxidation in muscle cells, both in vitro and in vivo, while displaying partial agonism in transactivation assays. PPARδ Agonist 10 is suitable for research focused on dyslipidemia and metabolic disorders. -
PPARγ Modulator
PPARγ modulator-1 is a non-agonistic modulator of the peroxisome proliferator-activated receptor gamma (PPARγ). It exhibits high binding affinity for PPARγ and inhibits kinase-mediated phosphorylation of this receptor. This compound is suitable for research applications focused on metabolic diseases, providing a means to study the effects of PPARγ modulation while potentially minimizing side effects associated with traditional agonists. -
PPARδ Agonist
L-783483 is a potent agonist of Peroxisome Proliferator-Activated Receptor delta (PPARδ). This compound has demonstrated the ability to reduce inflammation, as evidenced by its efficacy in attenuating Carrageenan-induced paw edema in murine models. L-783483 is useful in studies exploring metabolic disorders, inflammatory responses, and the therapeutic potential of PPARδ activation. -
PPARδ Agonist
PPARδ Agonist 11 is a selective agonist for peroxisome proliferator-activated receptor delta (PPARδ), exhibiting an EC50 of 20 nM. This compound effectively reduces nitrite oxide levels and pro-inflammatory cytokines, such as TNFα and IL-6, in LPS-stimulated RAW264.7 cells, demonstrating its anti-inflammatory activity through the NF-κB pathway. Additionally, PPARδ Agonist 11 shows good stability in human liver microsomes and plasma, and it alleviates Carrageenan-induced foot edema, making it a valuable tool for research in inflammation and metabolic disorders. -
PPARα/γ dual agonist
MHY908 is a potent dual agonist of peroxisome proliferator-activated receptors alpha (PPARα) and gamma (PPARγ). This compound enhances lipid metabolism and insulin sensitivity, making it a valuable tool in research related to metabolic disorders and obesity. Additionally, MHY908 inhibits melanogenesis by reducing the activity of mushroom tyrosinase, which may have implications in studies of pigmentation and skin biology. -
PPAR Modulator
CRX000227 is a PPAR modulator that selectively influences peroxisome proliferator-activated receptors (PPARs), playing a significant role in metabolic regulation. This compound demonstrates potential in the study of metabolic disorders and cell proliferation activities, making it a valuable tool for investigating the underlying mechanisms of various diseases related to metabolic dysfunction. Its utility in research applications may aid in the development of therapeutic strategies targeting metabolic and proliferative disorders.
