2. シグナル伝達
  3. Cell Cycle/DNA Damage
    Metabolic Enzyme/Protease
    Vitamin D Related/Nuclear Receptor
  4. PPAR
  5. PPARγ Isoform

PPARγ

PPARγ (Peroxisome Proliferator-Activated Receptor Gamma) is a ligand-activated nuclear receptor that functions as a central transcriptional regulator of adipocyte differentiation, lipid metabolism, insulin sensitivity, inflammation, and cellular energy homeostasis[1][2]. Mechanistically, PPARγ forms heterodimers with retinoid X receptors and regulates target gene expression through PPAR response elements, thereby coordinating metabolic and transcriptional programs that govern adipose tissue development and systemic glucose and lipid metabolism[3][4]. Because of its pivotal role in adipogenesis and insulin-responsive pathways, PPARγ has been extensively implicated in obesity, type 2 diabetes, metabolic syndrome, and related metabolic disorders[1][3]. In addition to metabolic regulation, PPARγ contributes to immune-cell maturation and function, particularly in macrophages and other inflammatory cell populations, linking metabolic signaling with inflammatory responses[4]. Compared with the related PPARα and PPARδ isoforms, which are predominantly associated with fatty acid oxidation and broader energy utilization pathways, PPARγ is distinguished by its dominant role in adipocyte differentiation and adipose tissue function[3]. Furthermore, alternative promoter usage and splicing generate multiple PPARG transcript variants, including γ1, γ2, and γ3, with evidence indicating isoform-specific regulation and distinct metabolic functions in different tissues[2][5]. For experimental applications, synthetic thiazolidinedione agonists activate PPARγ and improve insulin sensitivity, making them valuable pharmacological tools for investigating metabolic regulation, although their clinical use is limited by adverse effects such as weight gain[3][5].

製品番号 製品名 製品効果 純度
  • HY-14649
    Retinoic acid Agonist 99.81%
    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 99.94%
    Rosiglitazone (BRL 49653) is an orally active selective PPARγ agonist (EC50: 60 nM, Kd: 40 nM), with blood-brain barrier permeability. 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 99.98%
    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-15027
    5-Aminosalicylic Acid Agonist 99.97%
    5-Aminosalicylic acid (Mesalamine) acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB. 5-Aminosalicylic acid can inhibit the activity of osteopontin (OPN).
  • HY-13956
    Pioglitazone Activator 99.70%
    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-W012865
    Tartronic acid Activator ≥98.0%
    Tartronic acid, a dicarboxylic acid derive, is an inhibitor of the transformation of carbohydrates into fat under fat-deficient diet conditions. Tartronic acid promotes 3T3-L1 adipocyte differentiation by increasing the protein expression of FABP-4, PPARγ and SREBP-1. Tartronic acid promotes de novo lipogenesis and inhibits CPT-1β by upregulating acetyl-CoA and malonyl-CoA. Tartronic acid promotes weight gain and induces adipocyte hypertrophy in epididymal white adipose tissue and lipid accumulation in the livers of high-fat diet induced obese mice. Tartronic acid can be used for lipid metabolic disease research.
  • HY-122222
    MRL20 Agonist
    MRL20 is a PPARγ constitutive and allosteric agonist. MRL20 enhances the interaction between PPARγ and the co-activating peptide of TRAP220, with its EC50 being 10 nM. Even after being covalently blocked in the constitutive pocket by GW9662 (HY-16578) or T0070907 (HY-13202), MRL20 can still strengthen the interaction between PPARγ and TRAP220, with EC50 values of 176 and 440 nM respectively. MRL20 fails to completely inhibit its cell activation effect. MRL20 can be used to study the allosteric regulatory mechanism of PPARγ.
  • HY-181896S
    PPARγ agonist-23 Agonist
    PPARγ agonist-23 (Compound 9) is an orally active PPARγ agonist with an EC50 of 0.32 μM. PPARγ agonist-23 improves hepatic triglyceride levels, reduces scores of steatosis and hepatocellular ballooning, and decreases the total activity score of non-alcoholic steatohepatitis (NASH). PPARγ agonist-23 can be used for the research of non-alcoholic steatohepatitis.
  • HY-16995
    Pirinixic acid Agonist 99.34%
    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 99.78%
    Troglitazone is an orally active PPARγ agonist, with EC50s of 550 nM and 780 nM for human and murine PPARγ receptor, respectively. Troglitazone has anticancer activity, prevents and inhibits the development of type 2 diabetes.
  • HY-13202
    T0070907 Antagonist 99.98%
    T0070907 is a potent PPARγ antagonist with a Ki of 1 nM.
  • HY-N0019
    Daidzein Activator 99.81%
    Daidzein is a soy isoflavone, which acts as a PPAR activator.
  • 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-13861
    GW7647 Agonist 99.45%
    GW7647 is a potent PPARα agonist, with EC50s of 6 nM, 1.1 μM, and 6.2 μM for human PPARα, PPARγ and PPARδ, respectively.
  • HY-N0292
    Oleuropein Inhibitor 99.97%
    Oleuropein, found in olive leaves and oil, exerts antioxidant, anti-inflammatory and anti-atherogenic effects through direct inhibition of PPARγ transcriptional activity. Oleuropein induces apoptosis in breast cancer cells via the p53-dependent pathway and through the regulation of Bax and Bcl2 genes. Oleuropein also inhibits aromatase.
  • HY-B1773A
    Sodium propionate Activator 99.0%
    Sodium propionate is an orally active short-chain fatty acid. Sodium propionate can be produced by intestinal bacteria from the metabolism of dietary fiber. Sodium propionate increases PPAR-γ, inhibits NF-κB activation, and reduces COX-2 expression and NO production. Sodium propionate also induces Apoptosis and Autophagy. Sodium propionate reduces HSV-1-induced keratitis. Sodium propionate has anticancer effects against glioblastoma. Sodium propionate exhibits neuroprotective, antioxidant, and anti-inflammatory activities. Sodium propionate can be used in the research of spinal cord injury and Alzheimer's disease.
  • HY-N0163
    Magnolol Agonist 99.84%
    Magnolol, a natural lignan isolated from the stem bark of Magnolia officinalis, is a dual agonist of both RXRα and PPARγ, with EC50 values of 10.4 µM and 17.7 µM, respectively.
  • HY-17618
    Pemafibrate Agonist 99.85%
    Pemafibrate is a highly selective PPARα agonist, with an EC50 of 1 nM.
  • HY-N2302
    Fucoxanthin Inhibitor 99.38%
    Fucoxanthin (all-trans-Fucoxanthin) is a marine carotenoid and shows anti-obesity, anti-diabetic, anti-oxidant, anti-inflammatory and anticancer activities.
  • HY-N0393
    Glabridin Activator 99.98%
    Glabridin is a natural isoflavan from Glycyrrhiza glabra L., binds to and activates PPARγ, with an EC50 of 6115 nM. Glabridin exhibits antioxidant, anti-bacterial, anti-nephritic, anti-diabetic, anti-fungal, antitumor, anti-inflammatory, antiosteoporotic, cardiovascular protective, neuroprotective and radical scavenging activities.
製品番号 製品名 / Synonyms Species Source
製品番号 製品名 / Synonyms Application Reactivity