PPAR

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  1. Fenofibrate is a drug of the fibrate class. It is mainly used to reduce cholesterol levels in patients at risk of cardiovascular disease.
  2. Gemfibrozil (Lopid) is a compound used to lower lipid levels.
  3. PPARγ agonist

    5-Aminosalicylic acid (Mesalamine) acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB.
  4. 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.
  5. 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.
  6. Peroxisome Proliferator

    Cetaben is a unique, PPARα-independent peroxisome proliferator with hypolipidemic activity that inhibits cholesterol synthesis in the human hepatoma Hep-G2 cells resulting in reversible changes in Golgi morphology.
  7. PPARδ receptor agonist

    GW501516 (GW1516 or GSK-516) is a drug that acts as a PPARδ modulator.
  8. PPAR-γ antagonist

    T0070907 was identified as a potent and selective PPARgamma antagonist. With an apparent binding affinity (concentration at 50% inhibition of [(3)H]rosiglitazone binding or IC(50)) of 1 nm, T0070907 covalently modifies PPARgamma on cysteine 313 in helix 3 of human PPARgamma2.
  9. PPARγ agonist

    Pioglitazone selectively stimulates the nuclear receptor peroxisome proliferator-activated receptor gamma (PPAR-γ) and to a lesser extent PPAR-α.
  10. Ciprofibrate is a peroxisome proliferator-activated receptor agonist.
  11. PPARγ agonist

    Troglitazone is a selective PPARγ receptor agonist (EC50 values are 780 and 555 nM at murine and human PPARγ receptors respectively).
  12. PPARα agonist

    GW 7647 is a potent and highly selective PPARα agonist (EC50 values are 6, 1100 and 6200 nM for human PPARα, PPARγ and PPARδ receptors respectively).
  13. PPARδ agonist

    L-165,041 is a potent PPARδ agonist (Ki = 6 nM); displays > 100-fold selectivity for both mouse and human PPARδ receptors over other subtypes.
  14. PPARγ antagonist

    GW 9662 is a selective PPARγ antagonist (IC50 values are 3.3, 32 and 2000 nM for PPARγ, PPARα and PPARδ respectively).
  15. PPARα agonist

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

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

    GSK 0660 is a selective PPARβ antagonist (IC50 values are 0.155, > 10 and ??? 10 μM at PPARβ, PPARα and PPARγ respectively).
  18. PPARα antagonist

    GW6471 is a PPARα antagonist, shown to completely inhibit GW409544-induced activation of PPARα.
  19. PPAR-α/γ agonist

    Aleglitazar is a new dual PPAR-α/γ agonist with IC50 of 2.8 nM/4.6 nM.
  20. 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.
  21. PPARδ agonist

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

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

    GW0742 is a selective agonist of PPARδ with EC50 value of 1.1 nM.
  24. PPAR-γ partial agonist

    Balaglitazone is a novel partial agonist of PPAR-gamma (γ).
  25. 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.
  26. PPAR agonist

    GW1929 is a synthetic peroxisome proliferator-activated receptor-γ (PPARγ) agonist with IC50 of 6.2 nM and 13 nM for human and mouse, respectively.
  27. 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.
  28. PPAR agonist

    Elafibranor is an agonist of the peroxisome proliferator-activated Receptor-α and -δ, induces resolution of nonalcoholic steatohepatitis without fibrosis worsening.
  29. 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.
  30. PPAR agonist

    BMS-687453 is a potent and selective peroxisome proliferator activated receptor (PPAR) alpha agonist, with an EC(50) of 10 nM for human PPARalpha and approximately 410-fold selectivity vs human PPARgamma in PPAR-GAL4 transactivation assays.
  31. Fenofibric acid is a fibrate that acts as a lipid-lowering agent, decreasing low-density lipoprotein cholesterol and triglycerides.
  32. PPAR agonist

    Bezafibrate is the first clinically tested dual and pan-PPAR co-agonist.
  33. PPARγ Agonist

    CDDO-Im is a novel synthetic triterpenoid more potent than its parent compound CDDO both in vitro and in vivo; PPARγ Agonist.
  34. PPARβ/δ inverse agonist

    DG-172 is an orally active potent PPARβ/δ inverse agonist (IC50 = 26.9 nM). DG-172 inhibits Angptl4 gene expression in mouse myoblasts (IC50 = 9.5 nM) in vitro.
  35. PPARα agonist

    Clofibric acid is a PPARα agonist and hypolipidemic agent.
  36. PPARγ agonist

    Pioglitazone hydrochloride is a potent and selective PPARγ agonist with EC50s of 0.93 and 0.99 μM for human and mouse PPARγ, respectively.
  37. 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.
  38. penicillin binding protein inhibitor

    Cefminox Sodium, also known as Meicelin and MT-141, is a penicillin binding protein inhibitor used to treat bacterial infection.
  39. 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.
  40. 4'-Methoxychalcone regulates adipocyte differentiation through PPARγ activation. 4'-Methoxychalcone modulates the expression and secretion of various adipokines in adipose tissue that are involved in insulin sensitivity.
  41. PPARγ and CB2 receptor dual agonist

    VCE-004.8, a semi-synthetic multitarget cannabinoquinoid, is a specific PPARγ and CB2 receptor dual agonist with potent anti-inflammatory activity.
  42. PPAR gamma agonist

    Leriglitazone is a peroxisome proliferator activated receptor (PPAR) gamma agonist.
  43. PPAR-α antagonist

    NXT629 is a potent, selective, and competitive PPAR-α antagonist, with an IC50 of 77 nM for human PPARα, shows high selectivity over other nuclear hormone receptor, such as PPARδ, PPARγ, ERβ, GR and TRβ, IC50s are 6.0, 15, 15.2, 32.5 and >100 μM, respectively.
  44. PPAR γ agonist

    BR102375 is a non-TZD peroxisome proliferator-activated receptor γ (PPAR γ) full agonist for the treatment of type 2 diabetes, reveals EC50 value of 0.28?μM and Amax ratio?of 98%.
  45. PPARδ modulator

    MA-0204 is a potent, highly selective and orally available peroxisome proliferator activated receptor δ (PPARδ) modulator with EC50s of 0.4 nM, 7.9 nM and 10 nM for human, mouse and rat PPARδ, respectively. Potential treatment for Duchene Muscular Dystrophy (DMD).
  46. 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.
  47. PPARγ modulator

    GSK376501A is a selective peroxisome proliferator-activated receptor gamma (PPARγ) modulator for the treatment of type 2 diabetes mellitus.
  48. PPARδ agonist

    KD-3010 is a potent, orally active, and selective PPARδ agonist.
  49. PPAR-δ agonist

    Pparδ agonist 1 is a PPAR-δ agonist, with an EC50 of 5.06 nM, used in the research of PPAR-delta related diseases, such as mitochondrial diseases, muscular diseases, vascular diseases, demyelinating diseases and metabolic diseases.
  50. peptidoleukotrienes antagonist

    RG-12525 is a a specific, competitive and orally effective antagonist of the peptidoleukotrienes, LTC4, LTD4 and LTE4, inhibiting LTC4-, LTD4- and LTE4-inducd guinea pig parenchymal strips contractions, with IC50s of 2.6 nM, 2.5 nM and 7 nM, respectively; RG-12525 is also a peroxisome proliferator-activated receptor gamma (PPAR-gamma) agonist with IC50 of appr 60 nM and a potent inhibitor of CYP3A4, with a Ki value of 0.5 ?M.

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