PPAR

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  1. PPAR agonist

    Rosiglitazone maleate, an antidiabetic drug, works as an insulin sensitizer, by binding to the PPAR receptors in fat cells and making the cells more responsive to insulin.
  2. PPARγ agonist

    Troglitazone is a selective PPARγ receptor agonist (EC50 values are 780 and 555 nM at murine and human PPARγ receptors respectively).
  3. Gemfibrozil (Lopid) is a compound used to lower lipid levels.
  4. PPAR agonist

    Elafibranor is an agonist of the peroxisome proliferator-activated Receptor-α and -δ, induces resolution of nonalcoholic steatohepatitis without fibrosis worsening.
  5. PPAR agonist

    Rosiglitazone works as an insulin sensitizer, by binding to the PPAR receptors in fat cells and making the cells more responsive to insulin.
  6. PPARα antagonist

    GW6471 is a PPARα antagonist, shown to completely inhibit GW409544-induced activation of PPARα.
  7. Fenofibrate is a drug of the fibrate class. It is mainly used to reduce cholesterol levels in patients at risk of cardiovascular disease.
  8. PPARγ agonist

    5-Aminosalicylic acid (Mesalamine) acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB.
  9. PPARα antagonist

    GW 6471 is a potent PPARα antagonist.
  10. PPAR alpha agonist

    Pemafibrate, also known as (R)-K 13675, is a PPAR alpha agonist.
  11. PPAR agonist

    Saroglitazar is a novel peroxisome proliferator-activated receptor (PPAR) agonist with predominant PPARα and moderate PPARγ activity with EC50 values of 0.65 pM and 3 nM in HepG2 cells, respectively.
  12. PPAR-δ agonist

    Seladelpar (MBX-8025) is an orally active, potent (50% effect concentration EC50 2 nM), and specific PPAR-δ agonist.
  13. PTP1B/IKK-βinhibitor and dual PPARα and PPARβ agonist

    Ertiprotafib is an inhibitor of PTP1B, IkB kinase β (IKK-β), and a dual PPARα and PPARβ agonist, with an IC50 of 1.6 μM for PTP1B, 400 nM for IKK-β, an EC50 of ~1 μM for PPARα/PPARβ.
  14. PPARδ agonist

    Fonadelpar is a PPARδ agonist, used in the research of neuroparalytic keratopathy.
  15. PPAR alpha/gamma agonist

    Tesaglitazar is a dual peroxisome proliferator-activated receptor (PPAR) alpha/gamma agonist that is more potent on PPARγ than on PPARα, with EC50s of 13.4 μM and 3.6 μM for rat PPARα and human PPARα, respectively.
  16. PPARγ agonist

    Arhalofenate (MBX 102) is a selective partial agonist of peroxisome proliferator-activated receptor (PPAR)-γ, used for the treatment of type 2 diabetes.
  17. PPAR agonist

    Indeglitazar is an orally available peroxisome proliferator-activated receptor (PPAR) pan-agonist for all three PPAR subtypes alpha (α), delta (δ) and gamma (γ).
  18. PPARγ agonist

    Inolitazone a novel high-affinity PPARγ agonist that is dependent upon PPARγ for its biological activity with IC50 of 0.8 nM for growth inhibition.
  19. dual α/γ PPAR activator

    Peliglitazar racemate is the racemate of Peliglitazar. Peliglitazar is a novel dual α/γ PPAR activator.
  20. PPARγ agonist

    Sipoglitazar, also known as TAK-654, is a PPARγ agonist potentially for the treatment of diabetes.
  21. PPARγ Agonist

    Ciglitazone is a potent and selective agonist of the peroxisome proliferator-activated receptor gamma (PPARγ), with an EC50 of 3 μM. It effectively inhibits the proliferation and differentiation of Th17 cells and serves as a hypoglycemic agent in obese-hyperglycemic animal models. Additionally, Ciglitazone promotes apoptosis through the activation of p38 MAPK and facilitates the nuclear translocation of apoptosis-inducing factor (AIF) in opossum kidney (OK) renal epithelial cells, making it a valuable tool for research in metabolic and renal diseases.
  22. RNA RIBOTAC Degrader

    Dovitinib-RIBOTAC TFA is a targeted RNA RIBOTAC degrader that specifically binds to and degrades pre-miR-21. This compound demonstrates significant anti-tumor activity and effectively inhibits breast cancer metastasis. It serves as a valuable tool for research involving RNA-targeted degradation and its implications in cancer biology.
  23. PPAR Activator

    Bilobetin acts as a PPARα activator, enhancing lipid metabolism and insulin sensitivity. It effectively reduces blood lipid levels by promoting hepatic lipid uptake and oxidation, while decreasing triglyceride secretion and accumulation in tissues. Additionally, Bilobetin stimulates the phosphorylation and nuclear translocation of PPARα, resulting in increased cAMP levels and PKA activity. This compound is significant for research in metabolic disorders, particularly those related to insulin resistance and lipid regulation.
  24. MMP Inhibitor/PPARα Agonists

    Auraptene is an orally active geranyloxycoumarin compound naturally found in plants of the *Brassicaceae* family. It exhibits a wide range of biological activities, including antibacterial, anti-pathogenic, antioxidant, anti-tumor, and neuroprotective effects. Auraptene has shown therapeutic potential in the management of various chronic conditions such as hypertension and cystic fibrosis, making it a valuable compound for pharmacological and nutraceutical research.
  25. PPAR agonist

    Lobeglitazone sulfate is a novel thiazolidinedione and an orally active agonist of peroxisome proliferator-activated receptors (PPARs), with EC50 values of 137.4 nM for PPARγ and 546.3 nM for PPARα. It also acts as an inhibitor of the ERK/JNK/Smad/NF-κB signaling pathways. Lobeglitazone sulfate exhibits anti-inflammatory, anti-diabetic, anti-fibrotic, and anti-atherosclerotic activities, supporting its potential in the treatment of metabolic and inflammatory diseases.
  26. EGFR/PI3K Inhibitor

    MTX-531 is an orally active small molecule that inhibits EGFR (IC50 = 14.7 nM) and multiple PI3K isoforms, with IC50 values of 6.4 nM (PI3Kα), 233 nM (PI3Kβ), 8.3 nM (PI3Kγ), and 1.1 nM (PI3Kδ), demonstrating potent antitumor activity. Additionally, MTX-531 functions as a weak PPARγ agonist (IC50 = 2.5 µM), which may mitigate PI3K inhibitor-induced hyperglycemia.
  27. PPAR agonist

    Lobeglitazone is a novel thiazolidinedione-class compound and an orally active dual agonist of peroxisome proliferator-activated receptors (PPARs), with EC₅₀ values of 137.4 nM for PPARγ and 546.3 nM for PPARα. In addition to its metabolic effects, Lobeglitazone functions as an inhibitor of multiple pro-inflammatory and pro-fibrotic signaling pathways, including ERK, JNK, Smad, and NF-κB. Lobeglitazone exhibits a broad range of pharmacological activities, including anti-inflammatory, anti-diabetic, anti-fibrotic, and anti-atherosclerotic effects. These properties make it a promising candidate for therapeutic research in metabolic syndrome, type 2 diabetes, cardiovascular disease, and fibrosis-related conditions.
  28. PPAR δ/γ Agonist

    ZLY06 is a dual agonist of peroxisome proliferator-activated receptors (PPAR) δ and γ, exhibiting EC50 values of 341 nM and 237 nM, respectively. This compound promotes hepatic lipid accumulation through the inhibition of AKT1 phosphorylation, leading to the upregulation of CD36. Furthermore, ZLY06 enhances glucose and lipid metabolism while preventing weight gain, and mitigates fatty liver by facilitating β-oxidation of fatty acids and suppressing hepatic lipogenesis. It is valuable for research in metabolic disorders and fatty liver disease.
  29. PPARγ Activator

    12-Nitrolinoleate is a potent peroxisome proliferator-activated receptor γ (PPARγ) activator derived from linoleic acid through nitration. It effectively induces PPARγ-dependent gene expression in MCF-7 cells, demonstrating an EC50 of 0.045 μM. Additionally, 12-Nitrolinoleate exhibits anti-inflammatory properties by inhibiting NF-κB transcription in RAW 264.7 cells, along with reducing levels of pro-inflammatory cytokines such as IL-6, TNF-α, and CCL2 in response to LPS stimulation. This compound is valuable for research applications focused on metabolic regulation and inflammation.
  30. PPARγ Agonist

    Rosiglitazone hydrochloride is a selective agonist of the peroxisome proliferator-activated receptor gamma (PPARγ), demonstrating an EC50 of 60 nM and a Kd of 40 nM. In addition to its primary action, it acts as a TRPC5 activator with an EC50 of 30 μM and a TRPM3 inhibitor. This compound is extensively utilized in research related to obesity, diabetes, cellular senescence, and ovarian cancer.
  31. PPAR Activator

    Alpinetin is a flavonoid that acts as a PPAR-γ activator, demonstrating significant anti-inflammatory and hepatoprotective properties. It effectively inhibits lipopolysaccharide (LPS)-induced inflammation and protects against LPS-induced renal injury by modulating TLR4 expression and activating the Nrf2 pathway. Its diverse biological activities make Alpinetin a valuable reagent for research into tumor biology, cardiovascular health, and neuroprotection.
  32. Partial PPARγ Agonist

    Oroxin A is a partial agonist of the peroxisome proliferator-activated receptor gamma (PPARγ). It enhances PPARγ transcriptional activity through binding to the PPARγ ligand-binding domain. Additionally, Oroxin A demonstrates inhibitory effects on α-glucosidase and possesses antioxidant properties. Its anti-breast cancer potential is attributed to the induction of endoplasmic reticulum stress-mediated cellular senescence, making it a valuable tool for research in metabolic and cancer biology.
  33. PPAR Activator

    Angeloylgomisin H is a PPAR-γ activator derived from the lignin extract of Schisandra rubriflora. This compound has demonstrated the ability to enhance insulin-stimulated glucose uptake, making it a valuable candidate for research in metabolic disorders and diabetes. Its mechanism of action may provide insights into therapeutic strategies aimed at improving insulin sensitivity and glucose metabolism.
  34. PPARγ Agonist

    Ankaflavin is an orally active peroxisome proliferator-activated receptor gamma (PPARγ) agonist, derived from Monascus-fermented red rice. This compound demonstrates selective cytotoxicity in cancer cells, inducing apoptosis and facilitating cell death. Additionally, Ankaflavin exhibits notable anti-inflammatory, anti-cancer, anti-atherosclerotic, and hypolipidemic properties, making it useful for various research applications in cancer biology and metabolic disorders.
  35. PPAR Inhibitor

    AZ0108 is a selective inhibitor of poly(ADP-ribose) polymerases (PARPs), including PARP1, PARP2, PARP3, PARP6, TNKS1, and TNKS2. It displays potent inhibitory activity with IC50 values of <0.03 μM for PARP1 and PARP2, and exhibits significant biological effects such as preventing centrosome clustering with an EC50 of 0.053 μM. Additionally, AZ0108 demonstrates cytotoxicity in OCI-LY-19 cells, with a GI50 value of 0.017 μM, and shows favorable pharmacokinetic properties in rat and mouse models, making it a valuable tool for cellular and molecular biology research focused on DNA repair and cancer therapeutic studies.
  36. PPAR-1 Inhibitor

    AZD-9574-acid is a selective PPAR-1 inhibitor that serves as a crucial building block for the development of PROTAC molecules. Its inhibition of PPAR-1 demonstrates significant potential in the regulation of metabolic pathways and inflammatory responses. This compound is essential for researchers exploring targeted protein degradation and its applications in therapeutic development.
  37. PPARγ Agonist

    Rosiglitazone potassium is a selective PPARγ agonist with an EC50 of 60 nM and a Kd of 40 nM. This compound also acts as a TRPC5 activator (EC50: 30 μM) while inhibiting TRPM3. It is utilized in research investigating obesity, diabetes, cellular senescence, and ovarian cancer.
  38. PPARγ Agonist

    Pioglitazone potassium is a selective agonist of the peroxisome proliferator-activated receptor gamma (PPARγ), demonstrating high-affinity binding to the PPARγ ligand-binding domain with EC50 values of 0.93 μM and 0.99 μM for human and mouse PPARγ, respectively. This compound is commonly utilized in diabetes research to explore its effects on insulin sensitivity and glucose metabolism. Its action on PPARγ makes it a valuable tool for studying metabolic disorders and related therapeutic interventions.
  39. Selective PPARγ Agonist

    Pioglitazone-d4 is a deuterium-labeled derivative of Pioglitazone, a selective agonist of the peroxisome proliferator-activated receptor gamma (PPARγ). This compound demonstrates high affinity for the PPARγ ligand-binding domain, with EC50 values of 0.93 μM for human and 0.99 μM for mouse PPARγ. Pioglitazone-d4 is utilized in metabolic research to study insulin sensitivity, adipogenesis, and the mechanisms underlying type 2 diabetes mellitus.
  40. PPAR-α/γ and PPAR-γ Agonist

    Dehydroabietic acid is a diterpene resin acid that serves as a dual agonist for PPAR-α and PPAR-γ, with partial agonist activity at PPAR-γ. This compound exhibits significant biological activities, including anti-bacterial, anti-fungal, anti-inflammatory, and anti-cancer effects. It has been shown to mitigate insulin resistance and hepatic steatosis induced by high-fat diet consumption in animal models, making it a valuable reagent for research in metabolic disorders and inflammatory diseases.
  41. PPARα agonist

    WY 14643 is a highly potent PPARα agonist.
  42. PPAR antagonist

    GSK-3787 is a potent and selective peroxisome proliferator-activated receptor δ (PPARδ) antagonist (pIC50 = 6.6).
  43. PPARδ antagonist

    GSK 0660 is a selective PPARβ antagonist (IC50 values are 0.155, > 10 and ??? 10 μM at PPARβ, PPARα and PPARγ respectively).
  44. PPAR-α/γ agonist

    Aleglitazar is a new dual PPAR-α/γ agonist with IC50 of 2.8 nM/4.6 nM.
  45. PPARα/γ dual agonist

    Chiglitazar is a PPARα/γ dual agonist, with EC50s of 1.2, 0.08, 1.7 μM for PPARα, PPARγ and PPARδ, respectively.
  46. PPARδ agonist

    Pparδ agonist 2 is a PPARδ agonist extracted from patent WO 2016057656 A1.
  47. leukotriene biosynthesis inhibitor

    MK-886 is an inhibitor of leukotriene biosynthesis (IC50 = 3 nM in human polymorphonuclear leukocytes).
  48. PPAR agonist

    Lanifibranor, also known as IVA-337, is a peroxisome proliferator-activated receptors (PPAR) agonist.
  49. 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.
  50. penicillin binding protein inhibitor

    Cefminox Sodium, also known as Meicelin and MT-141, is a penicillin binding protein inhibitor used to treat bacterial infection.

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