Catalog No.
Product Name
Application
Product Information
Citations
-
PPAR-δ Agonist
Seladelpar Lysine dihydrate is a potent PPAR-δ agonist with an EC50 value of 2 nM. This compound exhibits significant specificity, demonstrating over 750-fold selectivity for PPAR-δ compared to PPARα and over 2500-fold selectivity relative to PPARγ. Research applications include the investigation of primary biliary cholangitis and the modulation of metabolic conditions, including the normalization of hyperglycemia, hyperinsulinemia, serum lipids, and cholesterol levels. Additionally, Seladelpar Lysine dihydrate has been shown to ameliorate nonalcoholic steatohepatitis in mouse models. -
PPARδ/γ Agonist
DB-959 is a potent agonist of the Peroxisome Proliferator-Activated Receptors delta (PPARδ) and gamma (PPARγ). It has been shown to enhance spatial learning and memory in mice models induced by Streptozotocin, indicating its potential therapeutic application in Alzheimer's disease. This compound is valuable for research focused on neurodegenerative disorders and metabolic regulation. -
PPAR Agonist
Deutaleglitazar is a selective agonist of dual peroxisome proliferator-activated receptors, PPARα and PPARγ. This compound exhibits significant biological activity in regulating lipid metabolism and glucose homeostasis, making it relevant for research in diabetes and metabolic syndrome. Its dual action supports investigations into therapeutic strategies for obesity-related conditions and cardiovascular diseases. -
PPARα Agonist
GW 590735 sodium is a selective agonist of peroxisome proliferator-activated receptor alpha (PPARα), known for its role in regulating lipid metabolism. This compound effectively elevates high-density lipoprotein (HDL) cholesterol levels while reducing low-density lipoprotein (LDL) and very low-density lipoprotein (VLDL) cholesterol, alongside a significant decrease in triglyceride levels. GW 590735 sodium demonstrates potential in research applications targeting dyslipidemia and metabolic disorders. -
PPARγ Agonist
PPARγ Agonist 10 is a selective agonist of the peroxisome proliferator-activated receptor gamma (PPARγ). It enhances insulin secretion, promotes glucose uptake, and improves insulin sensitivity in βTC6 cell lines. This compound is valuable for research in metabolic disorders, particularly type 2 diabetes and obesity, facilitating the study of PPARγ's role in glucose homeostasis and metabolic regulation. -
PPAR Agonist
Inolitazone hydrochloride hydrate is a high-affinity agonist of the peroxisome proliferator-activated receptor gamma (PPARγ), exhibiting an EC50 value significantly lower than that of Rosiglitazone. It selectively activates PPARγ without inhibiting RIE cells lacking this receptor. This compound is primarily utilized in cancer research, providing insights into the mechanisms of PPARγ in tumor biology and potential therapeutic applications. -
PPARγ Agonist
PPARγ Agonist 4 (Compound 18b) is a potent and selective agonist targeting the peroxisome proliferator-activated receptor gamma (PPARγ). This compound demonstrates notable antitumor activity specifically in combination with Imatinib, highlighting its potential in enhancing therapeutic effects in resistant tumor models. Furthermore, PPARγ Agonist 4 is non-cytotoxic to both resistant and non-resistant cell lines, making it a valuable tool for research applications aimed at understanding PPARγ modulation in cancer therapy. -
PPARδ Agonist
PPARδ Agonist 12 is a selective agonist of the peroxisome proliferator-activated receptor delta (PPARδ). This compound demonstrates the ability to inhibit the production of pro-inflammatory factors and nitric oxide. Additionally, PPARδ Agonist 12 effectively reduces macrophage infiltration at sites of inflammation, making it a valuable tool for studying inflammatory processes and their regulation in various research applications. -
PPAR Agonists
SB-219994 is a selective agonist of peroxisome proliferator-activated receptors (PPARs). It demonstrates potent anti-inflammatory activity by inhibiting airway neutrophilia and reducing associated chemoattractants and survival factors. This compound is valuable for research applications targeting inflammatory diseases and exploring the role of PPARs in immune responses. -
CB1 Antagonist/PPARα Agonist
OLHHA is a dual CB1 receptor antagonist and PPARα agonist. This compound demonstrates notable activity in inhibiting alcohol intake with an EC50 value of 0.2 mg/kg. Additionally, OLHHA effectively reduces hepatic lipid accumulation and circulating triglyceride levels, exhibiting anti-steatotic properties. Its mechanism and effects make it a valuable tool for research into non-alcoholic fatty liver disease (NAFLD). -
PPARα Agonist
Ciprofibrate Impurity A is a notable impurity of Ciprofibrate, which serves as a potent agonist of peroxisome proliferator-activated receptor alpha (PPARα). This compound enhances the phosphorylation levels of PPARα, thereby influencing lipid metabolism and glucose homeostasis. Ciprofibrate Impurity A is relevant for research applications focused on metabolic disorders, inflammation, and other PPARα-related signaling pathways. -
PPAR Agonist
BMS711939 is a selective agonist of peroxisome proliferator-activated receptor α (PPAR α), demonstrating an EC50 of 4 nM for human PPARα and 4.5 μM for human PPARγ. This compound shows promising pharmacokinetic properties in rat models and is known to elevate HDL cholesterol levels while decreasing LDL cholesterol and triglycerides. BMS711939 serves as a valuable tool for investigating lipid metabolism and the physiological effects of PPAR activation. -
PPAR Activator
Peliglitazar is a dual alpha and gamma peroxisome proliferator-activated receptor (PPAR) activator. It promotes insulin sensitivity and lipid metabolism, making it valuable in the study of metabolic disorders such as type 2 diabetes and obesity. Research applications include investigating the molecular mechanisms of PPAR signaling and developing therapeutic strategies for related conditions. -
PPAR-γ Agonist
MBX-102 acid is a selective partial agonist of PPAR-γ (Peroxisome Proliferator-Activated Receptor Gamma). This compound exhibits strong binding to plasma proteins, primarily serum albumin, which may influence its pharmacokinetics. MBX-102 acid is primarily utilized in research related to type 2 diabetes, aiding in the exploration of its role in glucose metabolism and insulin sensitivity. -
PPARγ Agonist
MRL20 is a PPARγ constitutive and allosteric agonist that enhances the interaction between PPARγ and the co-activating peptide TRAP220, exhibiting an EC50 of 10 nM. Notably, even when covalently inhibited in its constitutive pocket by GW9662 or T0070907, MRL20 can maintain its ability to facilitate the PPARγ-TRAP220 interaction, with subsequent EC50 values of 176 nM and 440 nM, respectively. This compound does not completely inhibit cell activation, making MRL20 a valuable tool for investigating the allosteric regulatory mechanisms of PPARγ in various biological contexts. -
PPAR Agonist
ZLY032 is a dual agonist of FFA1 and PPARδ, primarily targeting these important nuclear receptors involved in metabolic regulation. This compound demonstrates significant activity in enhancing glucose and lipid metabolism, offering potential benefits in alleviating liver fibrosis. ZLY032 is of particular interest for research applications related to metabolic disorders and liver health. -
Pparδ Agonist
Pparδ Agonist 7 is a highly potent agonist of peroxisome proliferator-activated receptor delta (Pparδ), a critical component in the regulation of metabolic homeostasis, inflammation, and cell growth and differentiation. This compound is particularly relevant for research applications related to non-alcoholic fatty liver disease (NAFLD). By modulating Pparδ activity, Pparδ Agonist 7 can provide insights into therapeutic strategies for metabolic disorders and associated inflammatory conditions. -
Pparδ Agonist
PPARδ Agonist 8 is a potent agonist targeting the peroxisome proliferator-activated receptor delta (PPARδ), a crucial member of the nuclear receptor transcription factor superfamily. This compound facilitates the regulation of metabolic homeostasis, inflammation, and cellular differentiation, making it valuable for studying various biological processes. PPARδ Agonist 8 shows promise in research related to non-alcoholic fatty liver disease (NAFLD), contributing to understanding and potential therapeutic strategies for metabolic disorders. -
ATX Inhibitor/PPARγ Agonist
EL244 is a dual inhibitor of Autotaxin (ATX), with an IC50 of 50 nM, and a selective agonist of PPARγ, exhibiting an IC50 of 1.3 μM. This compound shows low cytotoxicity in human HepG2 cells, with an EC50 of 81.2 μM, and minimal inhibition of the cardiac hERG potassium channel (12% at 25 μM). EL244 effectively reduces pulmonary Lysophosphatidic Acid (LPA) levels, mitigates fibrosis, and enhances respiratory function in vivo, making it a valuable tool for the study of idiopathic pulmonary fibrosis and interstitial lung disease (ILD). -
PPAR Agonist
E-3030 free acid is a potent dual agonist of peroxisome proliferator-activated receptor (PPAR) alpha and PPAR gamma. This compound demonstrates significant antidiabetic and lipid-modulating activities by effectively reducing blood glucose, triglycerides, non-esterified fatty acids, and insulin levels, while enhancing adiponectin levels. E-3030 has been shown to improve glucose tolerance and exhibit remarkable triglyceride and non-high-density lipoprotein cholesterol-lowering effects in various animal models, making it a valuable tool for metabolic research and drug discovery. -
PPARγ agonist
L-796449 is a potent agonist of the peroxisome proliferator-activated receptor gamma (PPARγ). It exhibits neuroprotective properties, making it valuable for investigating therapeutic strategies in stroke research. Its ability to activate PPARγ may provide insights into mechanisms underlying neuroinflammation and tissue preservation following ischemic events. -
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.
