1. Signaling Pathways
  2. Cell Cycle/DNA Damage
  3. PPAR

PPAR

Peroxisome proliferator-activated receptors

PPARs (Peroxisome proliferator-activated receptors) are ligand-activated transcription factors of nuclear hormone receptor superfamily comprising of the following three subtypes: PPARα, PPARγ, and PPARβ/δ. PPARs play essential roles in the regulation of cellular differentiation, development, and metabolism (carbohydrate, lipid, protein), and tumorigenesis of higher organisms. All PPARs heterodimerize with the retinoid X receptor (RXR) and bind to specific regions on the DNA of target genes. Activation of PPAR-α reduces triglyceride level and is involved in regulation of energy homeostasis. Activation of PPAR-γ enhances glucose metabolism, whereas activation of PPAR-β/δ enhances fatty acids metabolism.

Cat. No. Product Name Effect Purity
  • HY-14649
    Retinoic acid
    Agonist 99.74%
    Retinoic acid is a metabolite of vitamin A that plays important roles in cell growth, differentiation, and organogenesis. Retinoic acid is a natural agonist of RAR nuclear receptors, with IC50s of 14 nM for RARα/β/γ. Retinoic acid bind to PPARβ/δ with Kd of 17 nM. Retinoic acid acts as an inhibitor of transcription factor Nrf2 through activation of retinoic acid receptor alpha.
  • HY-17386
    Rosiglitazone
    Agonist 99.90%
    Rosiglitazone (BRL 49653) is an orally active selective PPARγ agonist (EC50: 60 nM, Kd: 40 nM). Rosiglitazone is an TRPC5 activator (EC50: 30 μM) and TRPM3 inhibitor. Rosiglitazone can be used in the research of obesity and diabetes, senescence, ovarian cancer.
  • HY-16578
    GW9662
    Antagonist 99.87%
    GW9662 is a potent and selective PPARγ antagonist with an IC50 of 3.3 nM, showing 10 and 1000-fold selectivity over PPARα and PPARδ, respectively.
  • HY-13956
    Pioglitazone
    Activator 99.66%
    Pioglitazone (U 72107) is an orally active and selective PPARγ (peroxisome proliferator-activated receptor) agonist with high affinity binding to the PPARγ ligand-binding domain with EC50 of 0.93 and 0.99 μM for human and mouse PPARγ, respectively. Pioglitazone can be used in diabetes research.
  • HY-N0182
    Fisetin
    Inhibitor 98.87%
    Fisetin is a natural flavonol found in many fruits and vegetables with various benefits, such as antioxidant, anticancer, neuroprotection effects.
  • HY-117727A
    Leriglitazone hydrochloride
    Agonist 99.58%
    Leriglitazone (Hydroxypioglitazone) hydrochloride, a metabolite of pioglitazone. Leriglitazone (Hydroxypioglitazone) hydrochloride PioOH is a PPARγ agonist, stabilizes the PPARγ activation function-2 (AF-2) co-activator binding surface and enhances co-activator binding, affording slightly better transcriptional efficacy. Leriglitazone (Hydroxypioglitazone) hydrochloride binds to the PPARγ C-terminal ligand-binding domain (LBD) with a Ki of 1.2 μM,Leriglitazone induces transcriptional efficacy of the PPARγ (LBD) with an EC50 of 680 nM.
  • HY-139040
    2-(Tetradecylthio)acetic acid
    Activator ≥98.0%
    2-Tetradecylthio acetic acid is a pan-peroxisome proliferator activated receptor (pan-PPAR) activator. 2-Tetradecylthio acetic acid induces hypolipidemia. 2-Tetradecylthio acetic acid reduces plasma lipids and enhances hepatic fatty acid oxidation in rodents. 2-Tetradecylthio acetic acid increases the expression of genes involved in fatty acid uptake, activation, accumulation, and oxidation.
  • HY-17386B
    Rosiglitazone potassium
    Agonist
    Rosiglitazone (BRL 49653) potassium is an orally active selective PPARγ agonist (EC50: 60 nM, Kd: 40 nM). Rosiglitazone potassium is a TRPC5 activator (EC50: 30 μM) and TRPM3 inhibitor. Rosiglitazone potassium can be used in the research of obesity and diabetes, senescence, ovarian cancer.
  • HY-17356
    Fenofibrate
    Agonist 99.92%
    Fenofibrate is a selective PPARα agonist with an EC50 of 30 μM. Fenofibrate also inhibits human cytochrome P450 isoforms, with IC50s of 0.2, 0.7, 9.7, 4.8 and 142.1 μM for CYP2C19, CYP2B6, CYP2C9, CYP2C8, and CYP3A4, respectively.
  • HY-15372
    GW6471
    Antagonist 98.81%
    GW6471 is a potent PPARα antagonist.
  • HY-13202
    T0070907
    Antagonist 99.98%
    T0070907 is a potent PPARγ antagonist with a Ki of 1 nM.
  • HY-16995
    Pirinixic acid
    Agonist 99.80%
    Pirinixic acid (Wy-14643) is a potent agonist of PPARα, with EC50s of 0.63 μM, 32 μM for murine PPARα and PPARγ, and 5.0 μM, 60 μM, 35 μM for human PPARα, PPARγ and PPARδ, respectively.
  • HY-50935
    Troglitazone
    Agonist 98.60%
    Troglitazone is a PPARγ agonist, with EC50s of 550 nM and 780 nM for human and murine PPARγ receptor, respectively.
  • HY-15027
    5-Aminosalicylic Acid
    Agonist ≥98.0%
    5-Aminosalicylic acid (Mesalamine) acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB.
  • HY-10838
    GW 501516
    Agonist 99.15%
    GW 501516 (GW 1516) is a PPARδ agonist with an EC50 of 1.1 nM.
  • HY-N0019
    Daidzein
    Activator 99.89%
    Daidzein is a soy isoflavone, which acts as a PPAR activator.
  • HY-16737
    Elafibranor
    Agonist 99.00%
    Elafibranor (GFT505) is a PPARα/δ agonist with EC50s of 45 and 175 nM, respectively.
  • HY-B2163
    Astaxanthin
    Activator ≥98.0%
    Astaxanthin, the red dietary carotenoid, is an orally effective and potent antioxidant. Astaxanthin inhibits NF-κB and down-regulates VEGF in blood glucose. Astaxanthin exerts anti-cancer cell proliferation, increases apoptosis, impairs migration and invasion by activating PPARγ and reducing the expression of STAT3. Astaxanthin also has neuroprotective and anti-inflammatory activity and can be used in studies of cancer, diabetic retinopathy, cardiovascular disease, and in the coloring of animal feed.
  • HY-N0014
    Icariin
    Activator 99.06%
    Icariin is a flavonol glycoside. Icariin inhibits PDE5 and PDE4 activities with IC50s of 432 nM and 73.50 μM, respectively. Icariin also is a PPARα activator.
  • HY-104049
    Lanifibranor
    Agonist 99.56%
    Lanifibranor is a pan peroxisome proliferator-activated receptor (PPAR) agonist with EC50s of 1.5, 0.87 and 0.21 μM for human PPARα, PPARσ and PPARγ, respectively.
Cat. No. Product Name / Synonyms Species Source

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