PPAR

Isoform-selective Products

Signaling Pathway

PPAR Signaling Pathway

PPAR Products

  • All (55)
  • PPAR Inhibitors (9)
  • PPAR Activators (13)
  • PPAR Antagonists (5)
  • PPAR Agonists (24)
  • PPAR Modulators (4)
  • New PPAR Products
Catalog No. Product Name Information Product Use Citations Product Validations
S2871 T0070907 T0070907 is a potent inhibitor of PPARγ (peroxisome proliferator activator receptor γ ) that induces G2/M arrest and enhances the effect of radiation in human cervical cancer cells through mitotic catastrophe. It also acts as an antagonist of PPARγ that suppresses breast cancer cell proliferation and motility via both PPARgamma-dependent and -independent mechanisms.
Nat Commun, 2024, 15(1):1429
Cell Discov, 2023, 9(1):54
Cell Discov, 2023, 9(1):54
S2556 Rosiglitazone Rosiglitazone is a potent antihyperglycemic agent and a potent thiazolidinedione insulin sensitizer with IC50 of 12, 4 and 9 nM for rat, 3T3-L1 and human adipocytes, respectively. Rosiglitazone is a pure ligand of PPAR-gamma, and has no PPAR-alpha-binding action. Rosiglitazone modulates TRP channels and induces autophagy. Rosiglitazone prevents ferroptosis.
Nat Commun, 2024, 15(1):1429
J Hematol Oncol, 2023, 16(1):30
EBioMedicine, 2023, 10.1016/j.ebiom.2023.104865
S2915 GW9662 GW9662 is a selective PPAR antagonist for PPARγ with IC50 of 3.3 nM in a cell-free assay, with at least 10- to 600-fold functional selectivity in cells with PPARγ versus PPARα and PPARδ.
J Hematol Oncol, 2024, 17(1):9
Int J Biol Sci, 2023, 19(11):3456-3471
Int J Biol Sci, 2023, 19(11):3456-3471
S2590 Pioglitazone Pioglitazone is a selective peroxisome proliferator-activated receptor-gamma (PPARγ) agonist, used to treat diabetes; A weak activator for full-length hPPARα, but not full-length hPPARδ.
Cell Rep, 2023, 42(7):112697
Gastroenterology, 2022, 162(4):1210-1225
Commun Biol, 2022, 5(1):231
S2505 Rosiglitazone maleate Rosiglitazone maleate, a member of the thiazolidinedione class of antihyperglycaemic agents, is a high-affinity selective agonist of the peroxisome proliferator-activated receptor-γ (PPAR-γ) with IC50 of 42 nM. Rosiglitazone maleate also modulates TRP channels and induces autophagy. Rosiglitazone prevents ferroptosis.
Stem Cell Reports, 2022, 17(11):2531-2547
Cell Death Dis, 2021, 12(11):972
Antioxidants (Basel), 2021, 10(2)155
S7484 FH535 FH535 is a Wnt/β-catenin signaling inhibitor and also a dual PPARγ and PPARδ antagonist.
Gastroenterology, 2023, S0016-5085(23)00114-2
Gastroenterology, 2023, 164(6):990-1005
Cell Death Dis, 2022, 13(5):493
S2075 Rosiglitazone HCl Rosiglitazone HCl is a blood glucose-lowering drugs, stimulating insulin secretion by binding to the PPAR receptors in fat cells.
Stem Cell Reports, 2022, 17(11):2531-2547
Cell Death Dis, 2021, 12(11):972
Antioxidants (Basel), 2021, 10(2)155
S8029 WY-14643 (Pirinixic Acid) WY-14643 (Pirinixic Acid, NSC 310038) is a potent and selective PPARα activator with an EC50 of 1.5 μM.
Cell Mol Gastroenterol Hepatol, 2022, 14(6):1311-1331
Front Pharmacol, 2022, 13:935937
Acta Biochim Biophys Sin (Shanghai), 2022, 54(2):220-231
S2798 GW6471 GW 6471 is a potent antagonist of PPARα with IC50 of 0.24 μM.
Oncogene, 2024, 43(6):406-419
Nat Commun, 2023, 14(1):6908
Nat Commun, 2023, 14(1):6908
S1794 Fenofibrate Fenofibrate is a compound of the fibrate class and fibric acid derivative. Fenofibrate is a selective agonist of PPARα with EC50 of 30 μM. Fenofibrate binds to and inhibits cytochrome P450 epoxygenase (CYP)2C with IC50 of 0.2 μM, 0.7 μM and 9.7 μM for CYP2C19, CYP2B6 and CYP2C9, respectively. Fenofibrate induces autophagy.
Cancer Lett, 2023, 10.1016/j.canlet.2023.216427
Cell Metab, 2022, 34(2):299-316.e6
Cancers (Basel), 2022, 14(2)282
S8025 GSK3787 GSK3787 is a selective and irreversible antagonist of PPARδ with pIC50 of 6.6, with no measurable affinity for hPPARα or hPPARγ.
Cell Discov, 2023, 9(1):54
Cell Discov, 2023, 9(1):54
J Cancer, 2023, 14(6):1049-1061
S2046 Pioglitazone HCl Pioglitazone HCl (AD-4833, U-72107E) is an inhibitor of cytochrome P450 (CYP)2C8 and CYP3A4 enzymes. Pioglitazone HCl inhibits CYP2C8, CYP3A4 and CYP2C9 with Ki of 1.7 μM, 11.8 μM and 32.1 μM, respectively. Pioglitazone HCl is also a selective peroxisome proliferator-activated receptor-gamma (PPARγ) agonist with EC50 of 0.93 μM and 0.99 μM for human PPARγ and mouse PPARγ, respectively. Pioglitazone HCl inhibits mitochondrial iron uptake, lipid peroxidation, and subsequent ferroptosis.
Commun Biol, 2022, 5(1):231
J Genet Genomics, 2022, S1673-8527(22)00133-3
J Cell Mol Med, 2022, 10.1111/jcmm.17154
S8020 GW0742 GW0742 is a potent and highly selective PPARβ/δ agonist, with IC50 of 1 nM, with 1000-fold selectivity over hPPARα and hPPARγ.
Life Sci, 2021, 279:119696
Cells, 2019, 8(12)
Int J Med Sci, 2019, 16(12):1593-1603
S7955 EPI-001 EPI-001 is an androgen receptor N-terminal domain antagonist with IC50 of ∼6 μM and a selective PPAR-gamma modulator.
Int J Mol Sci, 2023, 24(4)3823
Cell Death Dis, 2022, 13(7):626
Mar Drugs, 2022, 20(6)378
S7767 AZ6102 AZ6102 is a potent TNKS1/2 inhibitor that has 100-fold selectivity against other PARP family enzymes and shows IC50 of 5 nM for Wnt pathway inhibition in DLD-1 cells.
Nat Commun, 2022, 13(1):2070
Sci Adv, 2022, 8(19):eabh2332
Haematologica, 2021, 10.3324/haematol.2020.267096
S3834 Astaxanthin Astaxanthin (β-Carotene-4,4'-dione, Trans-Astaxanthin), a xanthophyll carotenoid, is a nutrient with unique cell membrane actions and diverse clinical benefits with excellent safety and tolerability. Astaxanthin, a red dietary carotenoid isolated from Haematococcus pluvialis, is a modulator of PPARγ and a potent antioxidant with antiproliferative, neuroprotective and anti-inflammatory activity.
Int Immunopharmacol, 2023, 119:110159
J Gerontol A Biol Sci Med Sci, 2022, 77-8:1485-1493
Aging (Albany NY), 2019, 11(22):10513-10531
S3846 Eupatilin Eupatilin (NSC 122413), a major flavonoid from Artemisia plants, possesses various beneficial biological effects including anti-inflammation, anti-tumor, anti-cancer, anti-allergy, and anti-oxidation activity. Eupatilin, a lipophilic flavonoid isolated from Artemisia species, is a PPARα agonist, and possesses anti-apoptotic, anti-oxidative and anti-inflammatory activities.
Int J Mol Sci, 2023, 24(6)5933
Front Pharmacol, 2022, 13:940475
Int J Mol Sci, 2022, 23(24)16055
S8432 Troglitazone Troglitazone is a potent agonist for the peroxisome proliferator-activated receptor-(PPAR) that is a ligand activated transcription factor regulating cell differentiation and growth. Troglitazone induces autophagy, apoptosis and necroptosis in bladder cancer cells. Troglitazone prevents RSL3-induced ferroptosis and lipid peroxidation in Pfa1 cells.
Free Radic Biol Med, 2021, 163:234-242
Biomed Pharmacother, 2020, 132:110741
Nat Commun, 2019, 11;10(1):4621
S5817 GSK0660 GSK0660 is a potent PPARβ/δ antagonist with a pIC50 of 6.8 (binding assay IC50 = 155 nM; antagonist assay IC50 = 300 nM) and is nearly inactive on PPARα and PPARγ with IC50s above approximately 10 μM.
Cells, 2024, 13(3):206.
Cells, 2024, 13(3)206
Elife, 2023, 12e82970
S4159 Bezafibrate Bezafibrate (BM 15075) is the first clinically tested dual and pan-PPAR co-agonism.
Nat Commun, 2021, 12(1):1929
PPAR Res, 2021, 2021:5589342
S9189 Oroxin A Oroxin A (Baicalein 7-O-glucoside), an active component isolated from the herb Oroxylum indicum (L.) Kurz, activates PPARγ and inhibits α-glucosidase, exerting antioxidant activity.
Front Pharmacol, 2022, 13:894899
An Acad Bras Cienc, 2022, 94(suppl 4):e20211400
S9723 CDDO-Im (RTA-403) CDDO-Im (RTA-403) is an activator of nuclear factor erythroid 2–related factor 2 (Nrf2) and peroxisome proliferator-activated receptor (PPAR). CDDO-Im binds to PPARα and PPARγ with Ki of 232 nM and 344 nM, respectively. CDDO-Im inhibits inflammatory response and tumor growth in vivo.
Ecotoxicol Environ Saf, 2022, 241:113754
Int J Mol Sci, 2022, 23(19)11715
S4527 Fenofibric acid Fenofibric acid (NSC 281318, Trilipix, FNF acid) is a fibrate that acts as a lipid-lowering agent, decreasing low-density lipoprotein cholesterol and triglycerides.
Front Med (Lausanne), 2021, 8:788663
Int J Pharm, 2019, 570:118661
S3868 Harmine Harmine (Telepathine), a fluorescent harmala alkaloid belonging to the beta-carboline family of compounds, is a highly cell-permeant and competitive inhibitor of ATP binding to the kinase pocket of DYRK1A, with about 60-fold higher IC50 value for DYRK2. Harmine also inhibits monoamine oxidases (MAOs), PPARγ and cdc-like kinases (CLKs). Harmine inhibits 5-HT2A serotonin receptor with Ki of 397 nM.
J Gerontol A Biol Sci Med Sci, 2022, 77-8:1485-1493
Cell Death Dis, 2019, 10(12):899
S4708 Palmitoylethanolamide Palmitoylethanolamide (PEA, Palmidrol, N-palmitoylethanolamine) is an endogenous fatty acid amide and selectively activates PPAR-α in vitro with an EC50 value of 3.1±0.4 μM.
Neurosci Insights, 2020, 15:2633105520975412
J Steroid Biochem Mol Biol, 2019, 10.1016/j.jsbmb.2018.07.005
S2665 Ciprofibrate Ciprofibrate (Win-35833) is a peroxisome proliferator-activated receptor agonist.
Respir Physiol Neurobiol, 2020, 271:103290
S1849 Daidzein Daidzein is a natural isoflavone phytoestrogen found in Leguminosae, used as a component of foods and dietary supplements. Daidzein is a soy isoflavone, which acts as a PPAR activator.
J Mol Neurosci, 2018, 64(2):211-223
S4207 Clofibric Acid Clofibric acid(Chlorofibrinic acid) is a PPARα agonist and hypolipidemic agent.
Lab Invest, 2023, 103(1):100004
S8770 Lanifibranor (IVA-337) Lanifibranor (IVA-337) is a moderately potent and well balanced pan PPAR agonist with EC50 values of 1537 nM, 866 nM and 206 nM for hPPARα, hPPARδ and hPPARγ, respectively.
Brain Res Bull, 2021, 177:22-30
S0531 DG172 dihydrochloride DG-172 dihydrochloride is a novel PPARβ/δ-selective antagonist with the IC50 of 27 nM.
Cell Signal, 2022, 93:110304
S6906 Capric acid Capric acid (DA, Decanoic acid, Decylic acid), a component of medium-chain triclycerides occurring naturally in coconut oil and palm kernel oil, contributes to seizure control through direct AMPA receptor inhibition. Capric acid is also a modulating ligand for PPARs. Due to its specific melting range the product may be solid, liquid, a solidified melt or a supercooled melt.
Pharmaceuticals (Basel), 2023, 16(5)692
S3786 Glabridin Glabridin (Q-100692, KB-289522, LS-176045), one of the active phytochemicals in licorice extract, binds to and activates the ligand binding domain of PPARγ, as well as the full length receptor. It is also a GABAA receptor positive modulator promoting fatty acid oxidation and improving learning and memory.
Life Sci, 2021, S0024-3205(20)31752-5
S3875 Alpinetin Alpinetin, a composition of Alpinia katsumadai Hayata, has been reported to have a number of biological properties, such as antibacterial, antitumor and other important therapeutic activities. Alpinetin is a flavonoid isolated from Alpinia katsumadai Hayata, activates activates PPAR-γ, with potent anti-inflammatory activity.
Nutrients, 2021, 13(10)3382
S3720 Elafibranor Elafibranor (GFT505) is an agonist of the peroxisome proliferator-activated receptor-α(PPAR-alpha) and peroxisome proliferator-activated receptor-δ(PPAR-δ). It improves insulin sensitivity, glucose homeostasis, and lipid metabolism and reduces inflammation.
JHEP Rep, 2023, 5(10):100845
S7867 Oleuropein Oleuropein is an antioxidant polyphenol isolated from olive leaf. Oleuropein exerts antioxidant, anti-inflammatory and anti-atherogenic effects and suppresses the adipocyte differentiation in vitro. Oleuropein inhibits PPARγ activity. Oleuropein exerts anti-adipogenic effect through direct inhibition of PPARγ transcriptional activity. Oleuropein also inhibits aromatase. Oleuropein induces apoptosis. Phase 2.
J Med Virol, 2019, 91(8):1440-1447
S9177 Gypenoside XLIX Gypenoside XLIX, a naturally occurring gynosaponin, is a selective peroxisome proliferator-activated receptor (PPAR)-alpha activator.
Am J Transl Res, 2023, 15(2):834-846
S1729 Gemfibrozil Gemfibrozil (CI-719) is an activator of peroxisome proliferator-activated receptor-alpha (PPARα), used for the treatment of hypercholesterolemia and hypertriglyceridemia.
S9199 Pseudoginsenoside F11 Pseudoginsenoside F11, a natural product found in American ginseng but not in Asian ginseng, is a novel partial PPARγ agonist.
S3290 Procyanidin B2 Procyanidin B2 (PCB2), a natural flavonoid found in commonly consumed foods, possess anti-inflammatory, anti-oxidant and anti-cancer activities. Procyanidin B2 activates PPARγ to induce M2 polarization in mouse macrophages. Procyanidin B2 significantly suppresses the activation of NLRP3 inflammasome in the lung tissue induced by paraquat in the rat model.
E0473 CUDA CUDA is a potent inhibitor of soluble epoxide hydrolase (sEH), with IC50s of 11.1 nM and 112 nM for mouse sEH and human sEH, respectively, also selectively increases peroxisome proliferator-activated receptor (PPAR) alpha activity.
S5121 Phytol Phytol (Trans-Phytol), a diterpene alcohol from chlorophyll widely used as a food additive and in medicinal fields, shows antinociceptive and antioxidant activities as well as anti-inflammatory and antiallergic effects. It is a specific activator of PPARα.
S0773 Mifobate Mifobate (SR-202), a potent and specific PPARγ antagonist, selectively inhibits Thiazolidinedione (TZD)-induced PPARγ transcriptional activity (IC50=140 μM).
E2876 pemafibrate Pemafibrate(K-877) is a selective agonist of peroxisome proliferator-activated receptor (PPAR) α with an IC50 of 10 µM.
E3521 Auricledleaf Swallowwort Root Extract Auricledleaf Swallowwort Root Extract is obtained from Cynanchum otophyllum Schneid., which may be mediated by activation of PPARα and TFEB, and the subsequent autophagy-lysosomal pathway enhancement, thus attenuate Alzheimer’s disease pathology and improve cognitive function in 3XTg mice.
S8046 GW7647 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.
S5824 Cinnamyl alcohol Cinnamyl alcohol is a naturally occurring compound that is found within cinnamon. Cinnamyl alcohol can be significantly attenuated the enhanced expression of obesity-related proteins PPARγ in MDI medium-cultivated 3T3-L1 cells.
S5113 Propyl gallate Propyl gallate (Gallic acid propyl esterZ, n-Propyl gallate) is an antioxidant used in foods especially animal fats and vegetable oils, also in a wide variety of cosmetics and beauty care products.
S3878 Bavachinin Bavachinin (7-O-Methylbavachin) is a novel natural pan-PPAR agonist from the fruit of the traditional Chinese glucose-lowering herb malaytea scurfpea. It shows stronger activities with PPAR-γ than with PPAR-α and PPAR-β/δ (EC50 = 0.74 μmol/l, 4.00 μmol/l and 8.07 μmol/l in 293T cells, respectively).
S0170 BMS-687453 BMS-687453 (compound 2) is a potent and selective agonist of PPARα with EC50 of 10 nM and IC50 of 260 nM for human PPARα.
S5812 Choline Fenofibrate Choline fenofibrate(ABT-335) is a newly developed choline salt of fenofibric acid, a synthetic phenoxy-isobutyric acid derivate with antihyperlipidemic activity that acts as an PPARα agonist.
S9674 Saroglitazar Saroglitazar (Lipaglyn, ZYH1) is an agonist of peroxisome proliferator-activated receptor (PPAR) with EC50 of 0.65 pM and 3 nM for hPPARα and hPPARγ in HepG2 cells, respectively.
S9129 20(S)-Ginsenoside Rh1 20(S)-Ginsenoside Rh1 (Prosapogenin A2, Sanchinoside B2, Sanchinoside Rh1) is one of major bioactive compounds extracted from red ginseng, which has been increasingly used for enhancing cognition and physical health worldwide. It exhibits potent characteristics of anti-inflammatory, antioxidant, immunomodulatory effects, and positive effects on the nervous system. Ginsenoside Rh1 inhibits the expression of PPAR-γ, TNF-α, IL-6, and IL-1β.
S9480 Raspberry Ketone Raspberry ketone (p-Hydroxybenzyl acetone, Frambinone, Oxyphenylon, Rheosmin, Rasketone) is a natural phenolic compound that is the primary aroma compound of red raspberries. Raspberry ketone shows cardioprotective action against isoproterenol-induced myocardial infarction in rats, and the effects may be due to its PPAR-α agonistic activity.
S5851 4'-Methoxychalcone 4'-Methoxychalcone, found in citrus, is chalcone derivative that has shown diverse pharmacological properties, including anti-tumor and anti-inflammatory activities. 4'-Methoxychalcone significantly enhanced adipocyte differentiation, in part, by its potent effects on PPARγ activation and by its reverse effect on TNF-α.
E1775New 2,4-Thiazolidinedione 2,4-Thiazolidinedione (Thiazolidinedione), an insulin sensitizer, is a specific agonist of peroxisome proliferator-activated receptor (PPAR)γ. Thiazolidinedione treatment corrects impaired muscle insulin action in vivo.
S2871 T0070907 T0070907 is a potent inhibitor of PPARγ (peroxisome proliferator activator receptor γ ) that induces G2/M arrest and enhances the effect of radiation in human cervical cancer cells through mitotic catastrophe. It also acts as an antagonist of PPARγ that suppresses breast cancer cell proliferation and motility via both PPARgamma-dependent and -independent mechanisms.
Nat Commun, 2024, 15(1):1429
Cell Discov, 2023, 9(1):54
Cell Discov, 2023, 9(1):54
S7484 FH535 FH535 is a Wnt/β-catenin signaling inhibitor and also a dual PPARγ and PPARδ antagonist.
Gastroenterology, 2023, S0016-5085(23)00114-2
Gastroenterology, 2023, 164(6):990-1005
Cell Death Dis, 2022, 13(5):493
S2798 GW6471 GW 6471 is a potent antagonist of PPARα with IC50 of 0.24 μM.
Oncogene, 2024, 43(6):406-419
Nat Commun, 2023, 14(1):6908
Nat Commun, 2023, 14(1):6908
S7767 AZ6102 AZ6102 is a potent TNKS1/2 inhibitor that has 100-fold selectivity against other PARP family enzymes and shows IC50 of 5 nM for Wnt pathway inhibition in DLD-1 cells.
Nat Commun, 2022, 13(1):2070
Sci Adv, 2022, 8(19):eabh2332
Haematologica, 2021, 10.3324/haematol.2020.267096
S4527 Fenofibric acid Fenofibric acid (NSC 281318, Trilipix, FNF acid) is a fibrate that acts as a lipid-lowering agent, decreasing low-density lipoprotein cholesterol and triglycerides.
Front Med (Lausanne), 2021, 8:788663
Int J Pharm, 2019, 570:118661
S7867 Oleuropein Oleuropein is an antioxidant polyphenol isolated from olive leaf. Oleuropein exerts antioxidant, anti-inflammatory and anti-atherogenic effects and suppresses the adipocyte differentiation in vitro. Oleuropein inhibits PPARγ activity. Oleuropein exerts anti-adipogenic effect through direct inhibition of PPARγ transcriptional activity. Oleuropein also inhibits aromatase. Oleuropein induces apoptosis. Phase 2.
J Med Virol, 2019, 91(8):1440-1447
S5824 Cinnamyl alcohol Cinnamyl alcohol is a naturally occurring compound that is found within cinnamon. Cinnamyl alcohol can be significantly attenuated the enhanced expression of obesity-related proteins PPARγ in MDI medium-cultivated 3T3-L1 cells.
S5113 Propyl gallate Propyl gallate (Gallic acid propyl esterZ, n-Propyl gallate) is an antioxidant used in foods especially animal fats and vegetable oils, also in a wide variety of cosmetics and beauty care products.
S9129 20(S)-Ginsenoside Rh1 20(S)-Ginsenoside Rh1 (Prosapogenin A2, Sanchinoside B2, Sanchinoside Rh1) is one of major bioactive compounds extracted from red ginseng, which has been increasingly used for enhancing cognition and physical health worldwide. It exhibits potent characteristics of anti-inflammatory, antioxidant, immunomodulatory effects, and positive effects on the nervous system. Ginsenoside Rh1 inhibits the expression of PPAR-γ, TNF-α, IL-6, and IL-1β.
S8029 WY-14643 (Pirinixic Acid) WY-14643 (Pirinixic Acid, NSC 310038) is a potent and selective PPARα activator with an EC50 of 1.5 μM.
Cell Mol Gastroenterol Hepatol, 2022, 14(6):1311-1331
Front Pharmacol, 2022, 13:935937
Acta Biochim Biophys Sin (Shanghai), 2022, 54(2):220-231
S9189 Oroxin A Oroxin A (Baicalein 7-O-glucoside), an active component isolated from the herb Oroxylum indicum (L.) Kurz, activates PPARγ and inhibits α-glucosidase, exerting antioxidant activity.
Front Pharmacol, 2022, 13:894899
An Acad Bras Cienc, 2022, 94(suppl 4):e20211400
S9723 CDDO-Im (RTA-403) CDDO-Im (RTA-403) is an activator of nuclear factor erythroid 2–related factor 2 (Nrf2) and peroxisome proliferator-activated receptor (PPAR). CDDO-Im binds to PPARα and PPARγ with Ki of 232 nM and 344 nM, respectively. CDDO-Im inhibits inflammatory response and tumor growth in vivo.
Ecotoxicol Environ Saf, 2022, 241:113754
Int J Mol Sci, 2022, 23(19)11715
S4708 Palmitoylethanolamide Palmitoylethanolamide (PEA, Palmidrol, N-palmitoylethanolamine) is an endogenous fatty acid amide and selectively activates PPAR-α in vitro with an EC50 value of 3.1±0.4 μM.
Neurosci Insights, 2020, 15:2633105520975412
J Steroid Biochem Mol Biol, 2019, 10.1016/j.jsbmb.2018.07.005
S1849 Daidzein Daidzein is a natural isoflavone phytoestrogen found in Leguminosae, used as a component of foods and dietary supplements. Daidzein is a soy isoflavone, which acts as a PPAR activator.
J Mol Neurosci, 2018, 64(2):211-223
S3875 Alpinetin Alpinetin, a composition of Alpinia katsumadai Hayata, has been reported to have a number of biological properties, such as antibacterial, antitumor and other important therapeutic activities. Alpinetin is a flavonoid isolated from Alpinia katsumadai Hayata, activates activates PPAR-γ, with potent anti-inflammatory activity.
Nutrients, 2021, 13(10)3382
S9177 Gypenoside XLIX Gypenoside XLIX, a naturally occurring gynosaponin, is a selective peroxisome proliferator-activated receptor (PPAR)-alpha activator.
Am J Transl Res, 2023, 15(2):834-846
S1729 Gemfibrozil Gemfibrozil (CI-719) is an activator of peroxisome proliferator-activated receptor-alpha (PPARα), used for the treatment of hypercholesterolemia and hypertriglyceridemia.
S3290 Procyanidin B2 Procyanidin B2 (PCB2), a natural flavonoid found in commonly consumed foods, possess anti-inflammatory, anti-oxidant and anti-cancer activities. Procyanidin B2 activates PPARγ to induce M2 polarization in mouse macrophages. Procyanidin B2 significantly suppresses the activation of NLRP3 inflammasome in the lung tissue induced by paraquat in the rat model.
E0473 CUDA CUDA is a potent inhibitor of soluble epoxide hydrolase (sEH), with IC50s of 11.1 nM and 112 nM for mouse sEH and human sEH, respectively, also selectively increases peroxisome proliferator-activated receptor (PPAR) alpha activity.
S5121 Phytol Phytol (Trans-Phytol), a diterpene alcohol from chlorophyll widely used as a food additive and in medicinal fields, shows antinociceptive and antioxidant activities as well as anti-inflammatory and antiallergic effects. It is a specific activator of PPARα.
E3521 Auricledleaf Swallowwort Root Extract Auricledleaf Swallowwort Root Extract is obtained from Cynanchum otophyllum Schneid., which may be mediated by activation of PPARα and TFEB, and the subsequent autophagy-lysosomal pathway enhancement, thus attenuate Alzheimer’s disease pathology and improve cognitive function in 3XTg mice.
S5851 4'-Methoxychalcone 4'-Methoxychalcone, found in citrus, is chalcone derivative that has shown diverse pharmacological properties, including anti-tumor and anti-inflammatory activities. 4'-Methoxychalcone significantly enhanced adipocyte differentiation, in part, by its potent effects on PPARγ activation and by its reverse effect on TNF-α.
S2915 GW9662 GW9662 is a selective PPAR antagonist for PPARγ with IC50 of 3.3 nM in a cell-free assay, with at least 10- to 600-fold functional selectivity in cells with PPARγ versus PPARα and PPARδ.
J Hematol Oncol, 2024, 17(1):9
Int J Biol Sci, 2023, 19(11):3456-3471
Int J Biol Sci, 2023, 19(11):3456-3471
S8025 GSK3787 GSK3787 is a selective and irreversible antagonist of PPARδ with pIC50 of 6.6, with no measurable affinity for hPPARα or hPPARγ.
Cell Discov, 2023, 9(1):54
Cell Discov, 2023, 9(1):54
J Cancer, 2023, 14(6):1049-1061
S5817 GSK0660 GSK0660 is a potent PPARβ/δ antagonist with a pIC50 of 6.8 (binding assay IC50 = 155 nM; antagonist assay IC50 = 300 nM) and is nearly inactive on PPARα and PPARγ with IC50s above approximately 10 μM.
Cells, 2024, 13(3):206.
Cells, 2024, 13(3)206
Elife, 2023, 12e82970
S0531 DG172 dihydrochloride DG-172 dihydrochloride is a novel PPARβ/δ-selective antagonist with the IC50 of 27 nM.
Cell Signal, 2022, 93:110304
S0773 Mifobate Mifobate (SR-202), a potent and specific PPARγ antagonist, selectively inhibits Thiazolidinedione (TZD)-induced PPARγ transcriptional activity (IC50=140 μM).
S2556 Rosiglitazone Rosiglitazone is a potent antihyperglycemic agent and a potent thiazolidinedione insulin sensitizer with IC50 of 12, 4 and 9 nM for rat, 3T3-L1 and human adipocytes, respectively. Rosiglitazone is a pure ligand of PPAR-gamma, and has no PPAR-alpha-binding action. Rosiglitazone modulates TRP channels and induces autophagy. Rosiglitazone prevents ferroptosis.
Nat Commun, 2024, 15(1):1429
J Hematol Oncol, 2023, 16(1):30
EBioMedicine, 2023, 10.1016/j.ebiom.2023.104865
S2590 Pioglitazone Pioglitazone is a selective peroxisome proliferator-activated receptor-gamma (PPARγ) agonist, used to treat diabetes; A weak activator for full-length hPPARα, but not full-length hPPARδ.
Cell Rep, 2023, 42(7):112697
Gastroenterology, 2022, 162(4):1210-1225
Commun Biol, 2022, 5(1):231
S2505 Rosiglitazone maleate Rosiglitazone maleate, a member of the thiazolidinedione class of antihyperglycaemic agents, is a high-affinity selective agonist of the peroxisome proliferator-activated receptor-γ (PPAR-γ) with IC50 of 42 nM. Rosiglitazone maleate also modulates TRP channels and induces autophagy. Rosiglitazone prevents ferroptosis.
Stem Cell Reports, 2022, 17(11):2531-2547
Cell Death Dis, 2021, 12(11):972
Antioxidants (Basel), 2021, 10(2)155
S2075 Rosiglitazone HCl Rosiglitazone HCl is a blood glucose-lowering drugs, stimulating insulin secretion by binding to the PPAR receptors in fat cells.
Stem Cell Reports, 2022, 17(11):2531-2547
Cell Death Dis, 2021, 12(11):972
Antioxidants (Basel), 2021, 10(2)155
S1794 Fenofibrate Fenofibrate is a compound of the fibrate class and fibric acid derivative. Fenofibrate is a selective agonist of PPARα with EC50 of 30 μM. Fenofibrate binds to and inhibits cytochrome P450 epoxygenase (CYP)2C with IC50 of 0.2 μM, 0.7 μM and 9.7 μM for CYP2C19, CYP2B6 and CYP2C9, respectively. Fenofibrate induces autophagy.
Cancer Lett, 2023, 10.1016/j.canlet.2023.216427
Cell Metab, 2022, 34(2):299-316.e6
Cancers (Basel), 2022, 14(2)282
S2046 Pioglitazone HCl Pioglitazone HCl (AD-4833, U-72107E) is an inhibitor of cytochrome P450 (CYP)2C8 and CYP3A4 enzymes. Pioglitazone HCl inhibits CYP2C8, CYP3A4 and CYP2C9 with Ki of 1.7 μM, 11.8 μM and 32.1 μM, respectively. Pioglitazone HCl is also a selective peroxisome proliferator-activated receptor-gamma (PPARγ) agonist with EC50 of 0.93 μM and 0.99 μM for human PPARγ and mouse PPARγ, respectively. Pioglitazone HCl inhibits mitochondrial iron uptake, lipid peroxidation, and subsequent ferroptosis.
Commun Biol, 2022, 5(1):231
J Genet Genomics, 2022, S1673-8527(22)00133-3
J Cell Mol Med, 2022, 10.1111/jcmm.17154
S8020 GW0742 GW0742 is a potent and highly selective PPARβ/δ agonist, with IC50 of 1 nM, with 1000-fold selectivity over hPPARα and hPPARγ.
Life Sci, 2021, 279:119696
Cells, 2019, 8(12)
Int J Med Sci, 2019, 16(12):1593-1603
S3846 Eupatilin Eupatilin (NSC 122413), a major flavonoid from Artemisia plants, possesses various beneficial biological effects including anti-inflammation, anti-tumor, anti-cancer, anti-allergy, and anti-oxidation activity. Eupatilin, a lipophilic flavonoid isolated from Artemisia species, is a PPARα agonist, and possesses anti-apoptotic, anti-oxidative and anti-inflammatory activities.
Int J Mol Sci, 2023, 24(6)5933
Front Pharmacol, 2022, 13:940475
Int J Mol Sci, 2022, 23(24)16055
S8432 Troglitazone Troglitazone is a potent agonist for the peroxisome proliferator-activated receptor-(PPAR) that is a ligand activated transcription factor regulating cell differentiation and growth. Troglitazone induces autophagy, apoptosis and necroptosis in bladder cancer cells. Troglitazone prevents RSL3-induced ferroptosis and lipid peroxidation in Pfa1 cells.
Free Radic Biol Med, 2021, 163:234-242
Biomed Pharmacother, 2020, 132:110741
Nat Commun, 2019, 11;10(1):4621
S4159 Bezafibrate Bezafibrate (BM 15075) is the first clinically tested dual and pan-PPAR co-agonism.
Nat Commun, 2021, 12(1):1929
PPAR Res, 2021, 2021:5589342
S2665 Ciprofibrate Ciprofibrate (Win-35833) is a peroxisome proliferator-activated receptor agonist.
Respir Physiol Neurobiol, 2020, 271:103290
S4207 Clofibric Acid Clofibric acid(Chlorofibrinic acid) is a PPARα agonist and hypolipidemic agent.
Lab Invest, 2023, 103(1):100004
S8770 Lanifibranor (IVA-337) Lanifibranor (IVA-337) is a moderately potent and well balanced pan PPAR agonist with EC50 values of 1537 nM, 866 nM and 206 nM for hPPARα, hPPARδ and hPPARγ, respectively.
Brain Res Bull, 2021, 177:22-30
S3786 Glabridin Glabridin (Q-100692, KB-289522, LS-176045), one of the active phytochemicals in licorice extract, binds to and activates the ligand binding domain of PPARγ, as well as the full length receptor. It is also a GABAA receptor positive modulator promoting fatty acid oxidation and improving learning and memory.
Life Sci, 2021, S0024-3205(20)31752-5
S3720 Elafibranor Elafibranor (GFT505) is an agonist of the peroxisome proliferator-activated receptor-α(PPAR-alpha) and peroxisome proliferator-activated receptor-δ(PPAR-δ). It improves insulin sensitivity, glucose homeostasis, and lipid metabolism and reduces inflammation.
JHEP Rep, 2023, 5(10):100845
S9199 Pseudoginsenoside F11 Pseudoginsenoside F11, a natural product found in American ginseng but not in Asian ginseng, is a novel partial PPARγ agonist.
E2876 pemafibrate Pemafibrate(K-877) is a selective agonist of peroxisome proliferator-activated receptor (PPAR) α with an IC50 of 10 µM.
S8046 GW7647 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.
S3878 Bavachinin Bavachinin (7-O-Methylbavachin) is a novel natural pan-PPAR agonist from the fruit of the traditional Chinese glucose-lowering herb malaytea scurfpea. It shows stronger activities with PPAR-γ than with PPAR-α and PPAR-β/δ (EC50 = 0.74 μmol/l, 4.00 μmol/l and 8.07 μmol/l in 293T cells, respectively).
S0170 BMS-687453 BMS-687453 (compound 2) is a potent and selective agonist of PPARα with EC50 of 10 nM and IC50 of 260 nM for human PPARα.
S5812 Choline Fenofibrate Choline fenofibrate(ABT-335) is a newly developed choline salt of fenofibric acid, a synthetic phenoxy-isobutyric acid derivate with antihyperlipidemic activity that acts as an PPARα agonist.
S9674 Saroglitazar Saroglitazar (Lipaglyn, ZYH1) is an agonist of peroxisome proliferator-activated receptor (PPAR) with EC50 of 0.65 pM and 3 nM for hPPARα and hPPARγ in HepG2 cells, respectively.
S9480 Raspberry Ketone Raspberry ketone (p-Hydroxybenzyl acetone, Frambinone, Oxyphenylon, Rheosmin, Rasketone) is a natural phenolic compound that is the primary aroma compound of red raspberries. Raspberry ketone shows cardioprotective action against isoproterenol-induced myocardial infarction in rats, and the effects may be due to its PPAR-α agonistic activity.
E1775New 2,4-Thiazolidinedione 2,4-Thiazolidinedione (Thiazolidinedione), an insulin sensitizer, is a specific agonist of peroxisome proliferator-activated receptor (PPAR)γ. Thiazolidinedione treatment corrects impaired muscle insulin action in vivo.
S7955 EPI-001 EPI-001 is an androgen receptor N-terminal domain antagonist with IC50 of ∼6 μM and a selective PPAR-gamma modulator.
Int J Mol Sci, 2023, 24(4)3823
Cell Death Dis, 2022, 13(7):626
Mar Drugs, 2022, 20(6)378
S3834 Astaxanthin Astaxanthin (β-Carotene-4,4'-dione, Trans-Astaxanthin), a xanthophyll carotenoid, is a nutrient with unique cell membrane actions and diverse clinical benefits with excellent safety and tolerability. Astaxanthin, a red dietary carotenoid isolated from Haematococcus pluvialis, is a modulator of PPARγ and a potent antioxidant with antiproliferative, neuroprotective and anti-inflammatory activity.
Int Immunopharmacol, 2023, 119:110159
J Gerontol A Biol Sci Med Sci, 2022, 77-8:1485-1493
Aging (Albany NY), 2019, 11(22):10513-10531
S3868 Harmine Harmine (Telepathine), a fluorescent harmala alkaloid belonging to the beta-carboline family of compounds, is a highly cell-permeant and competitive inhibitor of ATP binding to the kinase pocket of DYRK1A, with about 60-fold higher IC50 value for DYRK2. Harmine also inhibits monoamine oxidases (MAOs), PPARγ and cdc-like kinases (CLKs). Harmine inhibits 5-HT2A serotonin receptor with Ki of 397 nM.
J Gerontol A Biol Sci Med Sci, 2022, 77-8:1485-1493
Cell Death Dis, 2019, 10(12):899
S6906 Capric acid Capric acid (DA, Decanoic acid, Decylic acid), a component of medium-chain triclycerides occurring naturally in coconut oil and palm kernel oil, contributes to seizure control through direct AMPA receptor inhibition. Capric acid is also a modulating ligand for PPARs. Due to its specific melting range the product may be solid, liquid, a solidified melt or a supercooled melt.
Pharmaceuticals (Basel), 2023, 16(5)692
E1775New 2,4-Thiazolidinedione 2,4-Thiazolidinedione (Thiazolidinedione), an insulin sensitizer, is a specific agonist of peroxisome proliferator-activated receptor (PPAR)γ. Thiazolidinedione treatment corrects impaired muscle insulin action in vivo.

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