PPARβ/δ
PPARβ/δ (peroxisome proliferator-activated receptor β/δ) is a ligand-activated nuclear receptor that functions as a transcription factor through heterodimerization with retinoid X receptor (RXR), thereby regulating gene networks involved in cellular differentiation, survival, and energy metabolism[1]. Mechanistically, PPARβ/δ controls lipid utilization, fatty acid β-oxidation, glucose metabolism, mitochondrial function, and fuel switching, linking nutrient-derived lipid signals to transcriptional programs that maintain metabolic homeostasis[1][2][3]. Through both ligand-dependent and ligand-independent modes of transcriptional regulation, PPARβ/δ can activate, derepress, or repress target genes, highlighting its complex role in cellular adaptation and metabolic regulation[4][5]. In disease-related contexts, PPARβ/δ has been implicated in metabolic syndrome, cardiovascular disease, liver metabolic disorders, neuroinflammation, and neurodegeneration, where its regulatory effects on lipid metabolism and inflammatory pathways are considered biologically important[1][2][6]. Compared with related isoforms, PPARα predominantly regulates fatty acid oxidation in liver and other oxidative tissues, whereas PPARγ primarily controls adipogenesis and insulin sensitivity; in contrast, PPARβ/δ exhibits broader tissue distribution and plays a distinctive role in fuel utilization, mitochondrial biogenesis, and cardiac lipid metabolism[3][7][1]. For experimental applications, selective agonists such as GW0742 and GW501516 have been widely used to investigate PPARβ/δ-dependent metabolic and inflammatory responses, and PPARβ/δ agonism has been associated with enhanced fatty acid metabolism and altered substrate preference toward lipid utilization in preclinical models[6][8].
References:
- [1]. Rabezanahary H, et al. Live virus neutralizing antibodies against pre and post Omicron strains in food and retail workers in Québec, Canada. Heliyon. 2024 May 21;10(10):e31026. [Content Brief]
- [2]. Ngoi NY, et al. The redox-senescence axis and its therapeutic targeting. Redox Biol. 2021 Sep;45:102032. [Content Brief]
- [3]. Gilde AJ, et al. Peroxisome proliferator-activated receptor (PPAR) alpha and PPARbeta/delta, but not PPARgamma, modulate the expression of genes involved in cardiac lipid metabolism. Circ Res. 2003 Mar 21;92(5):518-24. [Content Brief]
- [4]. Adhikary T, et al. Genomewide analyses define different modes of transcriptional regulation by peroxisome proliferator-activated receptor-β/δ (PPARβ/δ). PLoS One. 2011 Jan 19;6(1):e16344. [Content Brief]
- [5]. Giordano Attianese GM, et al. Integrative and systemic approaches for evaluating PPARβ/δ (PPARD) function. Nucl Recept Signal. 2015 Apr 27;13:e001. [Content Brief]
- [6]. Strosznajder AK, et al. Recent Insights on the Role of PPAR-β/δ in Neuroinflammation and Neurodegeneration, and Its Potential Target for Therapy. Neuromolecular Med. 2021 Mar;23(1):86-98. [Content Brief]
- [7]. Lonardo A, et al. PPARs in molecular pathogenesis and drug treatment of type 2 diabetes-related MASLD. Explor Dig Dis. 2025;4:100590.
- [8]. Da'adoosh B, et al. Discovering highly selective and diverse PPAR-delta agonists by ligand based machine learning and structural modeling. Sci Rep. 2019 Jan 31;9(1):1106. [Content Brief]
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PPARβ/δ Related Products (45)
Related Products (45)
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NXT629
0 ImagesNXT629 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. NXT629 has potent anti-tumor activity and inhibits experimental metastasis of cancer cell in animal models.
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Seladelpar sodium
0 ImagesSynonyms: MBX-8025 sodium; RWJ-800025 sodiumSeladelpar (MBX-8025) sodium salt is an orally active, potent and specific PPARδ agonist with an EC50 of 2 nM. Seladelpar sodium salt shows more than 750-fold and 2500-fold selectivity over the PPARα and PPARγ receptors, respectively. Seladelpar sodium salt hydrochloride can be used for the study of primary biliary cholangitis.
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Norathyriol
0 ImagesNorathyriol (Mangiferitin) is a natural metabolite of Mangifera. Norathyriol inhibits α-glucosidase in a noncompetitive manner with an IC50 of 3.12 μM. Norathyriol inhibits PPARα, PPARβ, and PPARγ with IC50s of 92.8 µM, 102.4 µM, and 153.5 µM, respectively. Antioxidant, anticancer, antimicrobial, anti-inflammatory, anti-bacterial activities.
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F44-A13
0 ImagesCat. No.: HY-163436CAS No.: 1338190-14-9F44-A13 is an orally active and highly selective farnesoid X receptor (FXR) antagonist with an IC50 value of 1.1 μM. F44-A13 can optimize cholesterol metabolism and reduce its activity by inducing CYP7A1 expression. F44-A13 reduces levels of cholesterol, triglycerides, and low-density lipoprotein cholesterol (LDL-C) in mouse models. F44-A13 can be used in the study of metabolic diseases associated with lipid disorders.
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HWL-088
0 ImagesHWL-088 is a highly potent and orally active free fatty acid receptor 1 (FFA1/GPR40) agonist (EC50 of 18.9 nM) with moderate PPARδ activity (EC50 of 570.9 nM) . HWL-088 improves glucose and lipid metabolism, and has anti-diabetic effects.
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9(10)-Nitrooleate
0 ImagesSynonyms: 9(10)-Nitrated oleic acid9 (10)-Nitrooleate (9(10)-Nitrated oleic acid) is an endogenous lipid signaling mediator with vasoprotective effects. 9 (10)-Nitrooleate enhances enzymatic activity and improves nitric oxide bioavailability by inducing phosphorylation of Akt and ERK1/2, regulating the multi-site phosphorylation status of eNOS and optimizing its interaction with Hsp90. 9 (10)-Nitrooleate also activates PPARα, PPARδ and PPARγ receptors, thereby regulating adipogenesis, glucose uptake and inflammation-related gene expression, and exhibits immunosuppressive effects by inhibiting neutrophil migration and cytokine secretion. 9 (10)-Nitrooleate is widely used in studies of sepsis and related inflammatory diseases.
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PPAR agonist 5
0 ImagesCat. No.: HY-163547CAS No.: 3059387-62-8PPAR agonist 5 (compound 4b) is a potent PPAR agonist with EC50 values of 3.20, 1.51, 1.92 µM for PPARα, PPARβ/δ, PPARγ, respectively. PPAR agonist 5 shows anti-inflammatory effect.
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MA-0204
0 ImagesMA-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).
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E0924G
0 ImagesE0924G is an orally active activator for PPARδ with EC50 of 2.82 μM. E0924G promotes the upregulation of osteoprotegerin (OPG) with an EC50 of 0.29 μM. E0924G reduces RANKL-induced osteoclast differentiation and inhibites F-actin ring formation in RAW264.7 macrophages. E0924G regulates the bone density and bone loss in ovariectomized (OVX) and age-related osteoporosis models.
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Chiglitazar sodium
0 ImagesSynonyms: Carfloglitazar sodium
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Pioglitazone potassium
0 ImagesCat. No.: HY-13956BCAS No.: 1266523-09-4Synonyms: U 72107 potassiumPioglitazone (U 72107) potassium 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 μM and 0.99 μM for human and mouse PPARγ, respectively. Pioglitazone potassium can be used in diabetes research.
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Pparδ agonist 1
0 ImagesCat. No.: HY-107901CAS No.: 1902161-12-9Pparδ 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.
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Rac-Pemafibrate
0 ImagesCat. No.: HY-17618ACAS No.: 848258-31-1Synonyms: Rac-K13675Pemafibrate racemate (K13675 racemate) is the racemate of pemafibrate, and activates PPARα activity, with EC50s of 1 nM, >10 μM and 1.7 μM for h-PPARα, h-PPARγ and h-PPARδ, respectively.
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Fonadelpar
0 ImagesCat. No.: HY-17633CAS No.: 515138-06-4Synonyms: NPS-005; SJP-0035Fonadelpar is a PPARδ agonist, used in the research of neuroparalytic keratopathy.
