PPAR

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  1. PPARγ Partial Agonist

    PPARγ Agonist 2 is a potent partial agonist of the peroxisome proliferator-activated receptor gamma (PPARγ). This compound demonstrates significant biological activity in modulating glucose and lipid metabolism, making it an essential tool for studying metabolic diseases. It is particularly useful in research applications focused on obesity, diabetes, and cardiovascular disorders.
  2. PPAR Agonist

    PPARα/δ Agonist 3 is a selective agonist targeting peroxisome proliferator-activated receptors (PPARs), specifically activating PPARα, PPARδ, and PPARγ with EC50 values of 5.6 nM, 3.4 nM, and 1278 nM, respectively. This compound demonstrates significant anticholestatic activity in mouse models of cholestatic liver disease induced by ANIT or CDCA. It is useful for studying the role of PPAR activation in lipid metabolism and the pathophysiology of liver diseases.
  3. PPARγ Agonist

    PPARγ agonist-22 is a selective agonist of peroxisome proliferator-activated receptor gamma (PPARγ), which plays a crucial role in regulating glucose and lipid metabolism. This compound enhances cellular glucose uptake and decreases lipid accumulation in adipocytes, making it valuable in investigating metabolic disorders. PPARγ agonist-22 is particularly relevant for studies focused on the pathophysiology and treatment of type 2 diabetes.
  4. PPARγ Inhibitor, heme oxygenase-1 Activator, Nrf2 Activator

    PIISVYWK is a potent PPARγ inhibitor that also acts as an activator of heme oxygenase-1 (HO-1) and nuclear factor erythroid 2-related factor 2 (Nrf2). This compound effectively modulates the HO-1/Nrf2 signaling pathway, contributing to the reduction of oxidative stress and inflammation, while also exhibiting anti-obesity properties. PIISVYWK is suitable for research applications focused on obesity and related metabolic disorders.
  5. PPAR Modulator

    RB394 is a potent dual soluble epoxide hydrolase (sEH) and peroxisome proliferator-activated receptor gamma (PPARγ) modulator. This compound promotes adipocyte browning and demonstrates significant cardioprotective effects. RB394 is an invaluable tool for researchers studying metabolic syndrome and related metabolic disorders.
  6. PPARγ Agonist

    17-Oxo-4(Z),7(Z),10(Z),13(Z),15(E),19(Z)-docosahexaenoic acid is a PPARγ agonist that stimulates Nrf2-dependent antioxidant responses. This compound is a metabolite resulting from the lipoxygenase-mediated oxidation of docosahexaenoic acid (DHA). Its role in modulating PPARγ activity makes it relevant for research on metabolic diseases, inflammation, and antioxidant mechanisms.
  7. PPARγ Agonist

    CAY10410 is a potent agonist of peroxisome proliferator-activated receptor gamma (PPARγ). This compound effectively activates PPARγ in human B cells, promoting biological responses associated with lipid metabolism and inflammation, without inducing cytotoxicity in B lymphocytes. CAY10410 is valuable for research applications focused on metabolic disorders, immune modulation, and the role of PPARγ in various disease states.
  8. PPARδ Agonist

    LCI765 is a selective PPARδ agonist that demonstrates potent activity with an EC50 of 0.07 nM. This orally active compound is utilized in research focused on disorders related to energy homeostasis, including metabolic syndrome. It provides valuable insights into the pharmacological modulation of metabolic pathways and offers potential therapeutic avenues for related diseases.
  9. PPAR Agonist

    Mesalamine impurity P is an impurity derivative of Mesalamine, a specific agonist of the peroxisome proliferator-activated receptor gamma (PPARγ). This compound exhibits significant biological activity by inhibiting p21-activated kinase 1 (PAK1) and the nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB). It is utilized in research applications focusing on inflammatory bowel disease and metabolic disorders, contributing to the understanding of PPARγ modulation in therapeutic contexts.
  10. PPARα/γ agonist

    KRP-297 is a dual agonist of PPARα and PPARγ, targeting pathways involved in energy metabolism and lipid homeostasis. This compound has demonstrated the ability to restore lipid oxidation, while inhibiting excessive lipogenesis and triglyceride accumulation in hepatic tissue. KRP-297 is useful for research applications related to type 2 diabetes and dyslipidemia, providing insights into the modulation of metabolic disorders.
  11. PPAR Agonist

    KRP-101 is a selective PPARα agonist that modulates gene expression related to lipid metabolism. This compound significantly influences the regulation of genes such as apolipoprotein A-IV, which is implicated in the reduction of serum triglycerides and the elevation of HDL levels. KRP-101 is valuable for research focused on metabolic disorders and cardiovascular health.
  12. PPARγ Partial Agonist

    GW0072 is a partial agonist of peroxisome proliferator-activated receptor gamma (PPARγ), selectively inducing transcriptional activity without directly binding to the receptor's AF-2 helix. This unique mechanism allows for specific modulation of PPARγ activity and may influence pathways related to metabolism and inflammation. GW0072 is valuable for research investigating obesity, diabetes, and metabolic syndrome, as well as studying the broader roles of PPARγ in cellular regulation and differentiation.
  13. PPARα Ligand

    (E/Z)-Oleamide is a potent ligand for the peroxisome proliferator-activated receptor alpha (PPARα). This compound, derived from the plant Galium aparine L., plays a crucial role in modulating hippocampal plasticity through the transcriptional activation of cyclic AMP response element-binding protein (CREB). Its biological activities include the regulation of feeding and sexual behavior in rodent models, making it significant for research in neurobiology and metabolism.
  14. PPAR Agonist

    LY-510929 is a potent PPAR agonist that regulates gene expression involved in lipid metabolism and glucose homeostasis. It has been shown to induce left ventricular hypertrophy (LVH) under specific conditions, making it a valuable tool for research into cardiovascular diseases and metabolic disorders. This compound is utilized to investigate mechanisms of LVH and its associated biomarkers through various experimental techniques.
  15. PPARγ Agonist

    DN-108 is a thiazolidinedione derivative that serves as an orally active agonist for peroxisome proliferator-activated receptor γ (PPARγ). This compound exhibits notable antidiabetic properties, effectively improving hyperglycemia, hypertriglyceridemia, and hyperinsulinemia in diabetic mouse models. DN-108 enhances glucose uptake in tissues, such as increasing 2-deoxyglucose uptake in L6 muscle cells, and inhibits fatty acid synthase activity. This makes DN-108 a valuable tool for research focused on type 2 diabetes.
  16. PPARα Agonist

    PPARα Agonist 1 is a potent and selective agonist of the human peroxisome proliferator-activated receptor alpha (hPPARα). This compound modulates lipid metabolism and glucose homeostasis, making it valuable for research in metabolic disorders, cardiovascular diseases, and obesity. Its ability to activate PPARα allows for exploration of therapeutic strategies targeting metabolic regulation and inflammation.
  17. PPARγ Agonist

    VSP-77 is an orally active PPARγ agonist that enhances insulin sensitivity by inhibiting CDK5-mediated phosphorylation of PPARγ at Ser-273. This mechanism leads to the upregulation of key genes such as Glut4 and Adiponectin, which are crucial for glucose metabolism. In high-fat diet-induced diabetic mouse models, VSP-77 significantly improves glucose tolerance and lowers fasting blood glucose and insulin levels. It serves as a valuable reagent for studying diabetes and its associated metabolic pathways.
  18. PPAR Alpha Agonist

    K-111 is a potent oral PPAR alpha agonist that demonstrates significant efficacy in enhancing insulin sensitivity, promoting weight loss, and improving atherogenic dyslipidemia. This compound is valuable for research applications focused on type 2 diabetes, dyslipidemia, obesity, and metabolic syndrome. K-111's ability to modulate lipid metabolism and insulin resistance makes it an important tool for studying metabolic health and related disorders.
  19. PPARγ Activator

    4,5-DiHDPA lactone is a PPARγ activator and a derivative of docosahexaenoic acid (DHA). This compound has been shown to influence adipocyte differentiation and insulin sensitivity, making it valuable in metabolic research. Its ability to modulate PPARγ activity suggests potential applications in studying obesity and related metabolic disorders.
  20. PPAR Inhibitor

    Timcodar is a selective PPAR inhibitor that effectively blocks adipogenic transcriptional regulators, specifically PPARγ and C/EBPα, thereby reducing fat accumulation. Its mechanism of action mirrors that of rapamycin but without inducing immunosuppression or glucose resistance. Timcodar's significant impact on adipogenesis may offer a promising therapeutic avenue for addressing obesity, a growing global health concern. This compound is ideally suited for research related to metabolic disorders and obesity treatment strategies.
  21. PPARγ Agonist

    PPARγ Agonist 17 is a selective agonist of the peroxisome proliferator-activated receptor gamma (PPARγ). It enhances PPARγ activity, leading to cell cycle arrest in the G2/M phase, inhibition of cell migration, and induction of apoptosis in HT-29 colorectal cancer cells. This compound exhibits a broad spectrum of anti-proliferative effects against cancer cells while demonstrating relatively low toxicity in normal cells. Additionally, it is important to note that PPARγ Agonist 17 does not cross the blood-brain barrier, making it suitable for specific research applications.
  22. PPARγ Inhibitor

    PPARγ-IN-5 is a selective inhibitor of PPARγ, a key regulator of adipocyte differentiation and lipid metabolism. This compound effectively reduces lipid accumulation in hepatocytes, demonstrating minimal cytotoxicity at concentrations up to 400 µM in HepG2 cells. PPARγ-IN-5 is suitable for investigations into non-alcoholic fatty liver disease and related metabolic disorders.
  23. PPARγ Modulator

    YGT-31 is a selective modulator of peroxisome proliferator-activated receptor gamma (PPARγ) with an IC50 of 1.72 μM and a Ki of 0.62 μM. This compound has demonstrated the ability to lower blood glucose levels and enhance insulin sensitivity in db/db mouse models of type 2 diabetes by inhibiting CDK5-mediated phosphorylation at Ser273 of PPARγ. Additionally, YGT-31 exhibits protective effects against hepatic steatosis in non-alcoholic fatty liver disease (NAFLD) models, highlighting its potential in metabolic disease research.
  24. PPARδ Agonist

    PPARδ Agonist 9 is a potent agonist of the peroxisome proliferator-activated receptor delta (PPARδ), exhibiting an EC50 of 3.6 nM. This compound demonstrates significant in vivo efficacy, evidenced by its ability to lower serum levels of MCP-1 in murine models. Additionally, PPARδ Agonist 9 effectively inhibits the progression of atherosclerosis in the LDL receptor knockout mouse model, achieving an inhibition rate of 50-60%. This makes it a valuable tool for research into metabolic disorders and cardiovascular diseases.
  25. PPARγ Agonist

    PPARγ Agonist 7 is a selective full agonist of the peroxisome proliferator-activated receptor gamma (PPARγ) with an EC50 value of 4.34 μM. This compound effectively stimulates adiponectin production in human bone marrow mesenchymal stem cells (hBM-MSCs), making it a valuable tool for research into metabolic disorders and adipocyte differentiation. Its potent activation of PPARγ pathways highlights its potential applications in studying obesity, diabetes, and related metabolic syndromes.
  26. PPARα/γ Agonist

    PPARα/γ Agonist 2 is a potent oral activator of PPARα, functioning as a full agonist, and a partial agonist for PPARγ, with EC50 values of 0.95 μM and 0.91 μM, respectively. In addition to its dual agonistic activity, this compound serves as a PTP1B inhibitor, contributing to its role as an anti-diabetic agent. This reagent is essential for research into metabolic disorders, obesity, and type 2 diabetes, aiding in the exploration of therapeutic strategies targeting PPAR pathways.
  27. PPARδ Agonist

    PPARδ Agonist 13 is a highly selective and potent agonist for the peroxisome proliferator-activated receptor delta (PPARδ), demonstrating an EC50 of 0.50 nM. By binding to the PPARδ ligand-binding pocket, it effectively upregulates the expression of PPARδ target genes. This compound inhibits renal fibroblast activation, restores fatty acid oxidation, and mitigates TGF-β1-induced renal fibroblast activation, showcasing its anti-fibrotic effects in a mouse model of unilateral ureteral obstruction. PPARδ Agonist 13 serves as a valuable tool for investigating the mechanisms of renal fibrosis.
  28. PPARγ Modulator

    PPARγ modulator-2 is a reversible modulator of the peroxisome proliferator-activated receptor gamma (PPARγ), targeting its ligand-binding domain with an IC50 of 41 nM. This compound demonstrates significant biological activity by reducing blood glucose levels and enhancing glucose and insulin tolerance. Its efficacy has been validated in db/db mouse models, highlighting its potential applications in diabetes research and metabolic disorders.
  29. PPARα/γ Dual Agonist

    Chiglitazar sodium is a PPARα/γ dual agonist that exhibits EC50 values of 1.2 μM for PPARα, 0.08 μM for PPARγ, and 1.7 μM for PPARδ. This compound promotes the activation of both PPARα and PPARγ, making it relevant for studies focused on metabolic diseases and insulin sensitivity. Research applications include investigating the roles of PPAR receptors in lipid metabolism and glucose homeostasis.
  30. PPARα Agonist

    Elaidyl-sulfamide is a PPARα agonist that plays a significant role in regulating metabolic processes. This compound has been shown to reduce body weight gain and food intake, while also lowering circulating cholesterol levels. Additionally, Elaidyl-sulfamide increases glucose and insulin levels, making it a valuable tool for research into the mechanisms underlying obesity-related disorders.
  31. PPARβ/δ Antagonist

    PT-S58 is a PPARβ/δ antagonist exhibiting potent inhibitory activity with an IC50 value of 98 nM. This compound effectively blocks agonist-induced transcriptional activity of PPARβ/δ in vitro, making it a valuable tool for studying the functional roles of this receptor in various biological processes. Its application extends to research on metabolic disorders, inflammation, and cancer biology.
  32. PPAR-γ Agonistic Activities Compound

    Lyciumamide A is a compound with agonistic activity towards the peroxisome proliferator-activated receptor gamma (PPAR-γ), exhibiting EC50 values ranging from 10.09 to 44.26 μM. Additionally, it demonstrates inhibitory action on dipeptidyl peptidase-4 (DPP-IV) with an IC50 value of 47.13 μM. This compound holds potential for research applications targeting metabolic disorders and glucose homeostasis, highlighting its relevance in diabetes and obesity studies.
  33. PPAR α/PPAR γ Activator

    DRF-2519 free base is a dual activator of peroxisome proliferator-activated receptor alpha (PPAR α) and peroxisome proliferator-activated receptor gamma (PPAR γ). This compound exhibits significant antidiabetic and hypolipidemic activities, making it valuable for research into metabolic disorders. Its dual action on PPARs positions it as a significant tool in studies related to glucose metabolism and lipid regulation.
  34. PPAR-α Agonist

    Sitofibrate is a peroxisome proliferator-activated receptor alpha (PPAR-α) agonist, derived from Clofibrate. This compound exhibits antihyperlipidemic properties, facilitating the reduction of lipid levels in the bloodstream. Sitofibrate is utilized in research applications focused on metabolic disorders, cardiovascular diseases, and underlying mechanisms of lipid metabolism.
  35. PPAR Agonist

    Ketopioglitazone is a PPARγ agonist, serving as an active metabolite of the antidiabetic agent pioglitazone. It is primarily produced through the metabolism of pioglitazone by the cytochrome P450 isoform CYP2C8. Notably, ketopioglitazone has demonstrated efficacy in lowering blood glucose levels in a KKAy mouse model of type 2 diabetes, making it relevant for research into metabolic disorders and diabetes management.
  36. PPARγ Agonist

    PPARγ Agonist 9 is a selective agonist of the peroxisome proliferator-activated receptor gamma (PPARγ). This compound demonstrates significant biological activity by modulating PPARγ signaling pathways, which are critical in lipid metabolism and glucose homeostasis. It serves as a valuable tool in research applications focused on metabolic disorders, diabetes, and obesity-related studies.
  37. PPAR Activator

    17(S)-HDHA is a pro-resolving mediator that functions as a partial activator of peroxisome proliferator-activated receptors (PPARs), specifically PPARγ, PPARα, and PPARδ. Its biological activity is linked to the resolution of inflammation and modulation of metabolic processes. This compound is utilized in research to explore the roles of PPAR activation in anti-inflammatory responses and metabolic regulation.
  38. PPAR Agonist

    PPARα/γ agonist 5 is a dual agonist targeting peroxisome proliferator-activated receptors alpha and gamma, demonstrating notable biological activity at low concentrations. With EC50 values of 0.358 μM and 1.21 μM for PPARα and PPARγ, respectively, this compound shows promise in addressing type 2 diabetes and lipid metabolism disorders. Its potent efficacy supports its potential application in clinical development for metabolic health research.
  39. PPARα/δ Agonist

    (E/Z)-Elafibranor (also known as (E/Z)-GFT505) is a dual agonist of the peroxisome proliferator-activated receptors alpha (PPARα) and delta (PPARδ), exhibiting EC50 values of 45 nM and 175 nM, respectively. This compound plays a significant role in lipid metabolism and inflammation modulation, making it valuable for research in metabolic disorders, obesity, and non-alcoholic fatty liver disease (NAFLD). Its ability to simultaneously target multiple pathways positions (E/Z)-Elafibranor as a promising candidate for therapeutic interventions in metabolic diseases.
  40. PPARγ Agonist

    17-Oxo-7(Z),10(Z),13(Z),15(E),19(Z)-docosapentaenoic acid serves as a PPARγ agonist, primarily impacting inflammatory processes. This electrophilic oxo-derivative of docosahexaenoic acid (DHA) is produced in activated macrophages through a COX-2-catalyzed mechanism during inflammation. Its biological activity includes modulation of the NF-κB signaling pathway, inhibition of pro-inflammatory cytokine production, and reduction of nitric oxide synthesis, demonstrating significant anti-inflammatory properties. This compound is particularly valuable for research applications focused on inflammatory diseases and metabolic disorders.
  41. PPARα/PPARδ Agonist

    GW 2433 is a dual agonist of peroxisome proliferator-activated receptors alpha (PPARα) and delta (PPARδ). This compound exhibits the ability to enhance fatty acid uptake and metabolism, making it relevant for research in type II diabetes and dyslipidemia. It provides valuable insights into metabolic regulation and potential therapeutic strategies for metabolic disorders.
  42. PPAR-α Agonist

    ZINC17167211 is a potent agonist of peroxisome proliferator-activated receptor alpha (PPAR-α) with an EC50 of 0.16 nM. This compound is valuable for investigating metabolic disorders such as diabetes and hyperlipidemia, as well as inflammatory diseases. Its ability to activate PPAR-α makes it a useful tool for exploring therapeutic strategies aimed at modulating lipid metabolism and inflammation.
  43. PPAR-γ Inhibitor

    (±)-CBCQ is a potent inhibitor of PPAR-γ, exhibiting an EC50 value of 14.7 μM. This compound is of interest in research investigating the modulation of metabolic pathways and the potential therapeutic effects in obesity and diabetes. Its ability to interact with PPAR-γ makes it a valuable tool for studying the receptor's role in gene expression and lipid metabolism.
  44. PPARγ Agonist

    4-Oxo Docosahexaenoic Acid is a potent PPARγ agonist with notable antiproliferative properties. This compound effectively inhibits the growth of several triple-negative breast cancer cell lines, such as MDA-MB-231 and BT549, at concentrations of 50-100 μM, although it shows increased proliferation in MCF-7 cells. It covalently binds to PPARγ, activating gene transcription, as demonstrated in luciferase reporter assays and dendritic cells, with an EC50 of approximately 8-16 μM. This makes 4-Oxo DHA a valuable tool for research into cancer biology and PPARγ-associated pathways.
  45. PPARα/γ Agonist

    TZD18 is a potent dual agonist of PPARα and PPARγ, exhibiting IC50 values of 0.028 µM and 0.057 µM, respectively, while showing minimal activity toward PPARδ (>10 µM). This compound effectively reduces plasma glucose and triglyceride levels in diabetic mouse models. TZD18 holds promise for research into type 2 diabetes and related metabolic disorders.
  46. PPAR Agonist

    AVE-8134 is a potent agonist of the peroxisome proliferator-activated receptor alpha (PPARα). It exhibits an EC50 of 100 nM for the human PPARα receptor and 3000 nM for the rodent counterpart. This compound is used in research applications focused on metabolic regulation, lipid metabolism, and the modulation of inflammatory processes, making it a valuable tool for studies related to cardiovascular disease and metabolic disorders.
  47. PPAR α/γ Agonist

    CAY10514 is a dual agonist of peroxisome proliferator-activated receptors α (PPARα) and γ (PPARγ), exhibiting IC50 values of 0.173 μM and 0.642 μM, respectively. This compound is derived from 8(S)-HETE and demonstrates significant biological activity in modulating metabolic processes. CAY10514 is utilized in research applications related to metabolic disorders, obesity, and insulin sensitivity.
  48. PPAR-α Agonist

    ZINC08438472 is a selective agonist of peroxisome proliferator-activated receptor alpha (PPAR-α), demonstrating an EC50 value of 12.1 nM. This compound exhibits significant biological activity, making it a valuable tool in research focused on diabetes, hyperlipidemia, and inflammatory disorders. Its potent action on PPAR-α pathways offers potential insights into lipid metabolism and related therapeutics.
  49. PPARα/PPARγ Activator

    GW409544 is a highly potent activator of both PPARα and PPARγ, exhibiting EC50 values of 2.3 nM and 0.28 nM, respectively. This compound plays a significant role in the regulation of lipid metabolism and glucose homeostasis. GW409544 is instrumental for research investigating mechanisms underlying metabolic disorders and cardiovascular diseases, providing insights into potential therapeutic approaches.
  50. PPARγ Agonist

    CLX-0921 is an orally active PPARγ agonist, with an IC50 of 1.54 μM. It exhibits potent antihyperglycemic activity, making it a valuable tool for research in type 2 diabetes. This compound aids in the investigation of metabolic regulation and related therapeutic strategies in glucose homeostasis.

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