2. Signaling Pathways
  3. Cell Cycle/DNA Damage
    Metabolic Enzyme/Protease
    Vitamin D Related/Nuclear Receptor
  4. PPAR
  5. PPARδ Isoform

PPARδ

PPARδ (peroxisome proliferator-activated receptor delta, PPARD) is a ligand-activated nuclear receptor that functions as a transcription factor and regulates gene networks involved in lipid metabolism, glucose homeostasis, cellular differentiation, proliferation, and survival through heterodimerization with retinoid X receptor (RXR)[1][2]. Mechanistically, PPARδ integrates lipid-derived signaling with transcriptional control and modulates the expression of target genes in a ligand-dependent or ligand-independent manner, thereby influencing energy metabolism and cellular responses across multiple tissues[3][4]. PPARδ is particularly associated with fatty acid utilization, mitochondrial function, and metabolic adaptation, and its activity has been linked to the regulation of cardiac lipid metabolism and fuel switching in metabolically active tissues[5][6]. In disease models, PPARδ has been investigated in metabolic syndrome, cardiovascular disease, neuroinflammation, neurodegeneration, dyslipidemia, diabetes, and cancer, reflecting its broad physiological and pathological relevance[1][7]. Compared with related isoforms, PPARα primarily coordinates fatty-acid β-oxidation in liver and other oxidative tissues, whereas PPARγ is a master regulator of adipogenesis and insulin sensitivity; in contrast, PPARδ exhibits broader tissue distribution and distinct functions in energy metabolism, cell fate determination, and tissue-specific transcriptional regulation[1][3][6]. For experimental applications, selective PPARδ agonists are widely used to investigate metabolic regulation because receptor activation enhances fatty acid metabolism and promotes metabolic adaptations associated with improved energy utilization[7][8]. The availability of synthetic agonists and highly selective ligands has therefore made PPARδ a valuable target for mechanistic studies of metabolic and inflammatory pathways[1][8].

References:

Cat. No. Product Name Effect Purity
  • HY-N10361
    Drupanin
    		Activator 99.35%
    Drupanin is an orally active and selective AKR1C3 enzyme inhibitor and an RXRα agonist with an EC50 value of 4.8 μM, which is found in green propolis. Drupanin also activates PPARγ moderately. Drupanin induces adipogenesis and elevates aP2 mRNA levels in 3T3-L1 fibroblasts Drupanin has the potential for the research of breast and prostate cancers.
  • HY-Y1624
    1,1'-(Azodicarbonyl)-dipiperidine
    		Agonist ≥98.0%
    1,1'-(Azodicarbonyl)-dipiperidine (ADDP) can be used in the condensation reaction of alcohols with acidic compounds. 1,1'-(Azodicarbonyl)-dipiperidine can also be used in the synthesis of GPR120 agonists with antidiabetic activity, as well as the synthesis of triple agonists for PPARα, PPARγ, and PPARδ. 1,1'-(Azodicarbonyl)-dipiperidine can be used in metabolic disease research.
  • HY-21193
    Perfluoropentanoic acid
    		Modulator 98.0%
    Perfluoropentanoic acid (PFPeA), a short-chain perfluorinated compound, serves as an important indicator of perfluorinated compound pollution in ecosystems. Perfluoropentanoic acid exhibits certain toxicity to mice.
  • HY-168049
    ZLY06
    		Agonist 98.75%
    ZLY06 is an orally active dual agonist of peroxisome proliferator-activated receptor (PPAR) δ and γ (PPAR δ: EC50=341 nM; PPAR γ: EC50=237 nM). ZLY06 induces hepatic lipid accumulation by inhibiting the phosphorylation of AKT1, mediating the upregulation of CD36. In addition, ZLY06 significantly improves glucose and lipid metabolism without increasing body weight, and alleviates fatty liver by promoting β-oxidation of fatty acids and inhibiting hepatic lipogenesis.
  • HY-144111
    PPARα/δ agonist 1
    		Agonist 99.59%
    PPARα/δ agonist 1 is a potent PPARα/PPARδ dual agonist (PPARα EC50=7.0 nM; PPARδ EC50=8.4 nM). PPARα/δ agonist 1 is a high selectivity over PPARγ (PPARγ EC50=1316.1 nM). PPARα/δ agonist 1 has the potential for the research of nonalcoholic steatohepatitis.
  • HY-183318
    PPARα/δ agonist 4
    		Agonist
    PPARα/δ agonist 4 is a potent orally active and selective dual peroxisome proliferator-activated receptor (PPAR) α/δ agonist with EC50s of 0.36 and 1.31 nM, respectively. PPARα/δ agonist 4 exhibits >123-fold selectivity over PPARγ (EC50 = 160.84 nM). PPARα/δ agonist 4 upregulates expression of downstream fatty acid oxidation genes PDK4, CPT1A, and ACADVL. PPARα/δ agonist 4 can be used for the research of metabolic dysfunction-associated steatohepatitis.
  • HY-181652
    PPARδ agonist 13
    		Agonist
    PPARδ agonist 13 is a potent, selective and orally active PPARδ agonist with an EC50 values of 0.50 nM. PPARδ agonist 13 binds to the PPARδ ligand-binding pocket and upregulates PPARδ target gene expression. PPARδ agonist 13 inhibits renal fibroblast activation, restores fatty acid oxidation, and attenuates TGF-β1-induced renal fibroblast activation. PPARδ agonist 13 exhibits anti-renal fibrosis effects in a mouse model of unilateral ureteral obstruction. PPARδ agonist 13 can be used for the research of renal fibrosis.
  • HY-182619
    PPARα/δ antagonist-1
    		Antagonist
    PPARα/δ antagonist-1 is an orally active, highly selective dual antagonist of PPARα/δ, with IC50 values of 0.113 μM and 0.025 μM against human PPARα and PPARδ, respectively. PPARα/δ antagonist-1 exhibits an excellent in vitro activity profile and preliminary efficacy in mouse tumor models. PPARα/δ antagonist-1 can be used in studies related to cancers (melanoma metastasis, ovarian cancer).
  • HY-141494
    Pparδ agonist 5
    		Agonist
    Pparδ agonist 5, an orally active PPARδ-selective agonist (EC50=0.335 μM), is much greater than that of the prototypical standard GW0742. Pparδ agonist 5 promotes improvements in bone density and microarchitecture in vivo.
  • HY-172883
    ABP/PPAR modulator 1
    		Modulator
    ABP/PPAR modulator 1 is an orally active FABP and PPAR multiple modulator (IC50s of 0.65  μM and 1.08  μM for FABP1 and FABP4, EC50 s of 9.19  μM, 2.20  μM and 1.58 μM for PPARα, PPARγ and PPARδ). ABP/PPAR modulator 1 has potent anti-metabolic dysfunction-associated steatohepatitis (MASH) activity. ABP/PPAR modulator 1 dose-dependently ameliorates multiple pathological characteristics of fatty liver in WD + Carbon tetrachloride-induced MASH mice model.
  • HY-19522C
    Seladelpar (lysine dihydrate)
    		Agonist 99.51%
    Seladelpar Lysine dihydrate (MBX-8025 lysine dihydrate) is an orally active, selective PPAR-δ agonist with an EC50 of 2 nM against hPPAR-δ. Seladelpar Lysine dihydrate reduces serum IL-31 and bile acid levels. It alleviates pruritus symptoms. Seladelpar Lysine dihydrate enhances insulin sensitivity, normalizes levels of hyperglycemia, hyperinsulinemia, glucose disposal capacity, serum lipids and hepatic free cholesterol. It reduces steatosis, hepatic inflammation and improves liver fibrosis. Seladelpar Lysine dihydrate reverses the pathological changes of non-alcoholic steatohepatitis (NASH). It is applicable to research related to primary biliary cholangitis and non-alcoholic steatohepatitis (NASH).
  • 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.
  • 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.
  • HY-147757
    PPARγ/δ modulator 1
    		Modulator
    PPARγ/δ modulator 1 (compound 3e) is a potent PPAR modulator. PPARγ/δ modulator 1 is a PPARδ antagonist and a PPARγ partial agonist , with Ki values of 14.4 nM and 5.31 μM, respectively. PPARγ/δ modulator 1 has the EC50 of 7.3 and 12.6 μM for PPARδ corepression and adiponectin production, respectively.
  • HY-179015
    HSD17B13/PPAR modulator-1
    		Agonist
    HSD17B13/PPAR modulator-1 (Compound 17) is a HSD17B13/PPAR multitarget modulator. HSD17B13/PPAR modulator-1 is an inhibitor of HSD17B13, with its IC50 value being 0.91 μM. HSD17B13/PPAR modulator-1 is a PPAR agonist, with the EC50 values for PPARα, PPARδ, and PPARγ being 1.55, 0.12, and 0.01 μM respectively. HSD17B13/PPAR modulator-1 can significantly improve liver function, regulate lipid metabolism, alleviate fibrosis, and exert antioxidant and anti-inflammatory effects in the model of metabolic dysfunction-related steatohepatitis (MASH). HSD17B13/PPAR modulator-1 can be used for the study of MASH.
  • HY-176243
    15-Deoxy-Δ12,14-Prostaglandin J2-2-glyceryl ester
    		Agonist
    15-Deoxy-Δ12,14-Prostaglandin J2-2-glyceryl ester is a derivate of 15-Deoxy-Δ-12,14-prostaglandin J2 (HY-108568). 15-Deoxy-Δ-12,14-prostaglandin J2 (15d-PGJ2) is a cyclopentenone prostaglandin and a metabolite of PGD2. 15-Deoxy-Δ-12,14-prostaglandin J2 is a selective PPARγ (EC50 of 2 µM) and a covalent PPARδ agonist. 15-Deoxy-Δ-12,14-prostaglandin J2 promotes efficient differentiation of C3H10T1/2 fibroblasts to adipocytes with an EC50 of 7 μM.
  • HY-173217
    PPARα agonist 5
    		Agonist
    PPARα agonist 5 is an orally available, selective partial agonist of PPARα (EC50: 3 nM). PPARα agonist 5 reduces lipid accumulation and upregulates key PPARα target genes, exerting anti-fatty liver effects. PPARα agonist 5 also exhibits significant hypolipidemic and hypoglycemic effects through partial PPARγ agonist activity and mild inhibition of protein tyrosine phosphatase 1B (PTP1B) (IC50: 79.1 μM). PPARα agonist 5 has a good safety profile and can be used in the study of type 2 diabetes with dyslipidemia.
  • HY-121542
    PPARδ agonist 10
    		Agonist
    PPARδ agonist 10 (compound 7) is an orally active, selective, and partial agonist of PPARδ, with EC50 values of 0.053 μM and 0.30 µM for hPPARδ(LBD)-GAL4 and mPPARδ, respectively. PPARδ agonist 10 is a partial PPARδ agonist in transactivation assay but a full agonist on free fatty acids (FFA) oxidation in muscle cells both in vitro and in vivo. PPARδ agonist 10 can be used for dyslipidemia research.
  • HY-116597
    L-783483
    		Agonist
    L-783483 (F3MethylAA) is an agonist for PPARδ. L-783483 ameliorates Carrageenan (HY-125474)-induced paw edema in mice.
  • HY-168485
    PPARα/δ agonist 3
    		Agonist
    PPARα/δ agonist 3 (Compound 8) is the orally active agonist for PPAR, that activates PPARα, PPARδ and PPARγ with EC50s of 5.6, 3.4 and 1278 nM, respectively. PPARα/δ agonist 3 exhibits anticholestatic activity in mouse ANIT- or CDCA (HY-76847)-induced cholestatic liver disease models.
Cat. No. Product Name / Synonyms Species Source