1. Signaling Pathways
  2. Cell Cycle/DNA Damage
    Metabolic Enzyme/Protease
    Vitamin D Related/Nuclear Receptor
  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 Chemical Structure
  • 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.
    MRL20
  • 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.
    PPARγ agonist-23
  • HY-139175
    ZLY032
    Agonist
    ZLY032 is a dual FFA1/PPARδ agonist with the activity of improving glucose and lipid metabolism, alleviating liver fibrosis, and potentially inhibiting metabolic disorders.
    ZLY032
  • HY-143862
    Pparδ agonist 7
    Agonist
    Pparδ agonist 7 is a potent agonist of Pparδ. The peroxisome proliferator-activated receptor (PPAR) is a member of the intranuclear receptor transcription factor superfamily that plays a key role in the regulation of metabolic homeostasis, inflammation, cell growth and differentiation in vivo. Pparδ agonist 7 has the potential for the research of non-alcoholic fatty liver disease (NAFLD) (extracted from patent WO2019105234A1, compound TM4).
    Pparδ agonist 7
  • HY-143863
    PPARδ agonist 8
    Agonist
    Pparδ agonist 8 is a potent agonist of Pparδ. The peroxisome proliferator-activated receptor (PPAR) is a member of the intranuclear receptor transcription factor superfamily that plays a key role in the regulation of metabolic homeostasis, inflammation, cell growth and differentiation in vivo. Pparδ agonist 8 has the potential for the research of non-alcoholic fatty liver disease (NAFLD) (extracted from patent WO2021169769A1, compound TM2).
    PPARδ agonist 8
  • HY-124363
    5-cis Carbaprostacyclin
    Agonist
    5-cis Carbaprostacyclin is a stable analog of PGI2 based on Carbaprostacyclin (HY-112322). Carbacyclin is a PGI2 receptor agonist and vasodilator that activates PPARδ. 5-cis Carbaprostacyclin induces relaxation of pulmonary vascular tone.
    5-cis Carbaprostacyclin
  • HY-163432
    YGL-12
    Modulator
    YGL-12 is a potent PPARγ modulator with good binding affinity and an IC50 value of 0.85 μM. YGL-12 effectively blocks PPARγ Ser273 phosphorylation and can be used in diabetes research.
    YGL-12
  • HY-116028S1
    15-deoxy-Δ12,14-Prostaglandin D2-d4
    Activator
    15-Deoxy-Δ12,14-Prostaglandin D2-d4 (15-Deoxy-Δ12,14-PGD2-d4) is the deuterium labeled 15-deoxy-Δ12,14-Prostaglandin D2. 15-deoxy-Δ12,14-Prostaglandin D2 (15-Deoxy-Δ12,14-PGD2) is a metabolite of prostaglandin D₂ (PGD₂) (HY-101988), which can undergo further dehydration metabolism to 15-deoxy-Δ12,14-PGJ₂. 15-deoxy-Δ12,14-Prostaglandin D2 is a highly selective agonist for DP2 receptor and PPARγ. 15-deoxy-Δ12,14-Prostaglandin D2 causes morphological changes in eosinophils and migration of type II innate lymphoid cells (ILC2). 15-deoxy-Δ12,14-Prostaglandin D2 has a growth inhibitory effect on prostate cancer cells expressing PPARγ, induces cell cycle arrest and promotes apoptosis. 15-deoxy-Δ12,14-Prostaglandin D2 can be used in related research on asthma and prostate cancer.
    15-deoxy-Δ12,14-Prostaglandin D2-d<sub>4</sub>
  • HY-N18066
    Esculeogenin A
    Activator
    Esculeogenin A is the sapogenol of tomato saponin Esculeoside A (HY-N18067). Esculeogenin A is an orally active hepatoprotective, hypolipidemic, and antioxidant agent. Esculeogenin A regulates molecular targets like PPARα, SREBP1, Nrf2, NF-κB, ACAT1/ACAT2 to promote hepatic fatty acid oxidation, suppress de novo lipogenesis, enhance antioxidant defense, and inhibit inflammation. Esculeogenin A improves liver function, alleviates hyperlipidemia, and inhibits hepatic steatosis and foam cell formation, preventing nonalcoholic fatty liver disease in high-fat-diet-fed rats and reducing atherosclerotic lesions in apoE-deficient mice. Esculeogenin A can be used for the research of nonalcoholic fatty liver disease, atherosclerosis, and hyperlipidemia.
    Esculeogenin A
  • HY-179580
    EL244
    Agonist 99.55%
    EL244 is a dua Autotaxin (ATX) (IC50 = 50 nM) inhibitor and PPARγ (IC50 = 1.3 μM; Kd = 1.3 μM) agonist. EL244 demonstrates low cytotoxicity in human HepG2 cells (EC50 = 81.2 μM) with minimal inhibition of the cardiac hERG potassium channel (12% at 25 μM). EL244 significantly reduces pulmonary Lysophosphatidic Acid (LPA) levels, attenuates fibrosis, and restores respiratory function with limited systemic absorption in vivo. EL244 can be used for idiopathic pulmonary fibrosis and interstitial lung disease (ILD) research.
    EL244
  • HY-163443
    PPAR agonist 4
    Agonist
    PPAR agonist 4 (Compound 12) is an orally active agonist for peroxisome proliferator-activated receptor (PPAR), which activates PPARα, PPARδ and PPARγ with EC50s of 0.7, 0.7 and 1.8 μM, respectively. PPAR agonist 4 exhibits anti-liver fibrosis efficacy.
    PPAR agonist 4
  • HY-N7043R
    Isosilybin A (Standard)
    Agonist
    Isosilybin A (Standard) is the analytical standard of Isosilybin A (HY-N7043). Isosilybin A is a PPARγ agonist that can be isolated from silymarin. Isosilybin A activates extrinsic and intrinsic pathways of apoptosis through targeting of the Akt-NF-kB-AR axis. Isosilybin A can relieve the inflammatory response in the rosacea model via inhibiting Erk and p38 signaling pathways and M1 macrophage polarization, with its targets related to RELA and VEGFA. Isosilybin A has anti-prostate cancer (PCA) activity[1][2][3].
    Isosilybin A (Standard)
  • HY-117459
    E-3030 free acid
    Agonist
    E-3030 free acid is a potent dual activator of peroxisome proliferator-activated receptor (PPAR) alpha and PPARgamma, exhibiting significant antidiabetic and lipid-modulating effects. E-3030 decreases blood glucose, triglyceride, non-esterified fatty acids, and insulin levels, while increasing blood adiponectin levels. E-3030 improves glucose tolerance and shows remarkable triglyceride- and non-high-density lipoprotein cholesterol-lowering effects in animal models.
    E-3030 free acid
  • HY-173622
    PPARγ modulator-4
    Inhibitor
    PPARγ modulator-4 (Compound (I)) is a PPARγ inhibitor (KD: 3.75 μM). PPARγ modulator-4 can inhibit CDK5-mediated phosphorylation of PPARγ at Ser245. PPARγ modulator-4 can be used in insulin resistance research.
    PPARγ modulator-4
  • HY-123654
    L-796449
    Agonist
    L-796449 is a potent PPARγ agonist. L-796449 shows neuroprotective. L-796449 has the potential for the research of stroke.
    L-796449
  • HY-111775
    LJ570
    Agonist
    LJ570 is a PPARα/PPARγ dual agonist with EC50s of 1.05 and 0.12 μM, respectively.
    LJ570
  • HY-155062
    IR-251
    Inhibitor
    IR-251 is a mitochondrion-targeting NIR fluorescent probe. IR-251 targets mitochondria via OATPs and causes mitochondrial damage in tumor cells. IR-251 IR-251 induced ROS overproduction by inhibiting PPARγ, and then inhibiting the β-catenin signaling pathway and downstream protein molecules related to the cell cycle and metastasis. IR-251 inhibits tumor proliferation and metastasis.
    IR-251
  • HY-170581
    PPARγ/δ modulator 2
    Modulator
    PPARγ/δ modulator 2 (Compound 3h) is a PPARγ agonist and PPARδ antagonist. The Ki values for PPARγ and PPARδ are 2.8 μM and 43 nM, respectively. PPARγ/δ modulator 2 significantly enhances the production of Adiponectin and promotes adipogenic differentiation of human bone marrow mesenchymal stem cells (hBM-MSCs). PPARγ/δ modulator 2 can be used in the study of metabolic disorders associated with hypoadiponectinemia.
    PPARγ/δ modulator 2
  • HY-N7687
    Caulophyllogenin
    Agonist
    Caulophyllogenin is a triterpene saponin extracted from M. polimorpha. Caulophyllogenin is a partial PPARγ agonist, with an EC50 of 12.6 μM. Caulophyllogenin can be used for the research of type-2 diabetes, obesity, metabolic syndrome and inflammation.
    Caulophyllogenin
  • HY-180398
    PA-082
    Modulator
    PA-082 is a selective PPAR-γ modulator that functions as a partial agonist. PA-082 causes partial recruitment of SRC1, TIF2, SRC3 and full recruitment of PGC1-α to PPAR-γ ligand-binding domain. PA-082 prevents triglyceride accumulation during de novo adipogenesis and antagonizes Rosiglitazone (HY-17386)-induced lipid accumulation. PA-082 potentiates insulin-stimulated glucose uptake in adipocytes and protects against TNFα-induced insulin resistance. PA-082 can be used for the research of type 2 diabetes.
    PA-082
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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