PPARα
PPARα is a ligand-activated nuclear receptor that controls fatty acid metabolism in oxidative tissues, especially liver, heart, and muscle[1]. Mechanistically, hepatocyte PPARα acts as a lipid sensor that coordinates fasting-responsive gene networks for fatty acid homeostasis, ketogenesis, and metabolic adaptation[2]. In disease models, liver PPARα protects against NAFLD by supporting whole-body fatty acid homeostasis, while combined PPARα and PPARβ/δ activation improves steatosis, inflammation, and fibrosis in preclinical liver disease models[3][1]. Compared with related isoforms, PPARα primarily promotes fatty acid catabolism, whereas PPARγ favors fatty acid uptake, triglyceride storage, insulin sensitivity, and glucose metabolism[4][5]. For experimental applications, fibrates and WY-14,643 serve as PPARα agonists, while GW6471 supports antagonist-based studies by stabilizing corepressor recruitment to the PPARα ligand-binding domain[6][7].
References:
- [1]. Pawlak M, et al. Molecular mechanism of PPARα action and its impact on lipid metabolism, inflammation and fibrosis in non-alcoholic fatty liver disease. J Hepatol. 2015 Mar;62(3):720-33. [Content Brief]
- [2]. Fougerat A, et al. Lipid sensing by PPARα: Role in controlling hepatocyte gene regulatory networks and the metabolic response to fasting. Prog Lipid Res. 2024 Nov;96:101303. [Content Brief]
- [3]. Montagner A, et al. Liver PPARα is crucial for whole-body fatty acid homeostasis and is protective against NAFLD. Gut. 2016 Jul;65(7):1202-14. [Content Brief]
- [4]. Wang YX. PPARs: diverse regulators in energy metabolism and metabolic diseases. Cell Res. 2010 Feb;20(2):124-37. doi: 10.1038/cr.2010.13. Epub 2010 Jan 26. PMID: 20101262; PMCID: PMC4084607. et al. PPARs: diverse regulators in energy metabolism and metabolic diseases. Cell Res. 2010 Feb;20(2):124-37. [Content Brief]
- [5]. Montaigne D, et al. PPAR control of metabolism and cardiovascular functions. Nat Rev Cardiol. 2021 Dec;18(12):809-823. [Content Brief]
- [6]. Oike Y, et al. Angiopoietin-like proteins: potential new targets for metabolic syndrome therapy. Trends Mol Med. 2005 Oct;11(10):473-9. [Content Brief]
- [7]. Xu HE, et al. Structural basis for antagonist-mediated recruitment of nuclear co-repressors by PPARalpha. Nature. 2002 Feb 14;415(6873):813-7. [Content Brief]
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PPARα Related Products (139)
Related Products (139)
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Recombinant Proteins (2)
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Antibodies (1)
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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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ESP-31015
0 ImagesCat. No.: HY-107054CAS No.: 413624-55-2Synonyms: ETC-1001ESP-31015 (ETC-1001) is an orally active and non-fibrate based PPARα agonists. ESP-31015 demonstrates significant lipid-regulating effects in the obese Zucker rat model. ESP-31015 can be used in cardiovascular disease research.
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Imiglitazar
0 ImagesCat. No.: HY-101649CAS No.: 250601-04-8Synonyms: TAK-559Imiglitazar (TAK559) is a potent and dual human PPARα and PPARγ1 agonist with EC50 values of 67 and 31 nM.
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AU403
0 ImagesCat. No.: HY-184474AU403 is a potent, brain-penetrant, isoform-selective LXRβ/PPARδ dual agonist (EC50 ≈ 45 nM for LXRβ and EC50 ≈ 40 nM for PPARδ). AU403 is designed to bypass LXRα-driven hepatotoxicity. AU403 significantly improves cognitive functions and reduces amyloid-β plaque burden in 3xTg-AD mice. AU403 is a promising dual-acting agonist for the research of Alzheimer’s disease.
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AZD4619
0 ImagesCat. No.: HY-113820CAS No.: 549494-39-5AZD4619 is an orally active, selective peroxisome proliferator-activated receptor α (PPARα) agonist. AZD4619 increases alanine aminotransferase 1 (ALT1) protein expression in a dose-dependent manner in human, but not in rat primary hepatocytes. AZD4619 is a lipid-lowering drug.
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XYQ3-B11
0 ImagesCat. No.: HY-181894CAS No.: 3126891-03-7
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Cevoglitazar
0 ImagesCat. No.: HY-19848CAS No.: 839673-52-8Synonyms: LBM-642
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HSD17B13/PPAR modulator-1
0 ImagesCat. No.: HY-179015HSD17B13/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.
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PPARα/δ agonist 4
0 ImagesCat. No.: HY-183318CAS No.: 3108258-69-8PPARα/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.
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Romazarit
0 ImagesCat. No.: HY-106027CAS No.: 109543-76-2Synonyms: RO 31-3948
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(E)-Osmundacetone (Standard)
0 ImagesCat. No.: HY-N1966RCAS No.: 123694-03-1(E)-Osmundacetone (Standard) is the analytical standard of (E)-Osmundacetone (HY-N1966). This product is intended for research and analytical applications. (E)-Osmundacetone is an inhibitor of the MAPK pathway. (E)-Osmundacetone inhibits the activation of the MAPK signaling pathway and restores the expression of PPARα/ACOX1. (E)-Osmundacetone abrogates abnormal cell proliferation, migration and liver metastasis induced by PTPRO silencing in colorectal cancer cells. (E)-Osmundacetone blocks OA-RD17-mediated activation of the MAPK signaling pathway, thereby reducing macrophage proliferation and migration. (E)-Osmundacetone is applicable to relevant research on colorectal cancer.
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GW-9820
0 ImagesCat. No.: HY-123125CAS No.: 195131-60-3GW9820 is PPARα and PPARγ activator (EC50s: 0.37 μM for PPARα; 0.288 μM for PPARγ). GW9820 increases CLA-1. GW9820 can be used in the research of atherosclerosis.
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PPARα agonist 5
0 ImagesCat. No.: HY-173217PPARα 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.
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KRP-105
0 ImagesCat. No.: HY-19852CAS No.: 876145-69-6KRP-105 is a potent, highly selective, and orally effective PPAR alpha (EC50 = 8 nM) agonist. KRP-105 can significantly reduce serum triglyceride, total cholesterol, and non high density lipoprotein cholesterol levels. KRP-105 can be used for research on metabolic diseases such as dyslipidemia.
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DN203316
0 ImagesCat. No.: HY-162963CAS No.: 2982696-04-6Synonyms: PPARδ agonist 11DN203316 (PPARδ agonist 11) is a potent, selective, orally active PPARδ agonist (EC50 = 20 nM) with high selectivity over PPARα and PPARγ. DN203316 suppresses NF-κB-mediated inflammatory signaling, inhibits ferroptosis by upregulating xCT and GPX4, and attenuates STING-TBK1-IRF3-driven fibrogenic responses. DN203316 is useful for research on inflammatory disorders, metabolic dysfunction-associated steatohepatitis (MASH), and liver fibrosis.
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PPARα/δ agonist 3
0 ImagesCat. No.: HY-168485CAS No.: 3050611-33-8
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Dehydroepiandrosterone sulfate sodium (Standard)
0 ImagesSynonyms: DHEA sulfate sodium (Standard); Prasterone sulfate sodium (Standard)Dehydroepiandrosterone sulfate (DHEA sulfate; Prasterone sulfate) sodium salt (Standard) is the analytical standard of Dehydroepiandrosterone sulfate sodium salt (HY-B0765). This product is intended for research and analytical applications. Dehydroepiandrosterone sulfate (DHEA sulfate; Prasterone sulfate) is a neurosteroid and the main secretion product of the adrenal gland. Dehydroepiandrosterone sulfate has both non-competitive antagonist activity of GABAA receptor and agonist activity of σ1 receptor. Dehydroepiandrosterone sulfate can partially penetrate the blood-brain barrier, inhibit GABAA receptor-mediated chloride influx, enhance NMDA receptor activity through σ1 receptors, exert anti-inflammatory, anti-glucocorticoid and antidepressant effects, and increase convulsive sensitivity. Dehydroepiandrosterone sulfate participates in neuroprotection, neurite growth regulation and catecholamine secretion regulation, and can be used in the study of depression, post-traumatic stress disorder (PTSD), Alzheimer's disease, etc. Dehydroepiandrosterone sulfate may also be a biomarker for cardiovascular disease mortality, and its concentration is independently and negatively correlated with mortality.
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(E/Z)-Oleamide
0 ImagesSynonyms: Octadec-9-enamide(E/Z)-Oleamide (Octadec-9-enamide) is a PPARα ligand in hippocampal nuclei. (E/Z)-Oleamide can be isolated from plant Galium aparine L. (GA). (E/Z)-Oleamide controls hippocampal plasticity via transcriptional activation of CREB, and regulates feeding and sexual behavior in rats.
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PPARα agonist 1
0 ImagesCat. No.: HY-146733CAS No.: 3032632-02-0PPARα agonist 1 is a potent and full hPPARα agonist.
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Ciprofibrate (Standard)
0 ImagesSynonyms: Win35833 (Standard)Ciprofibrate (Standard) is the analytical standard of Ciprofibrate. This product is intended for research and analytical applications. Ciprofibrate (Win35833) is a potent peroxisome proliferator and increases the phosphorylation level of the PPARalpha. Ciprofibrate acts as an orally active hypolipidaemic agent and can be used for the research of primary hyperlipidaemias.
