PPAR

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PPAR Signaling Pathway Map

PPAR Signaling Pathways

PPAR Products

  • All (50)
  • PPAR Inhibitors (9)
  • PPAR Activators (11)
  • PPAR Antagonists (4)
  • PPAR Agonists (22)
  • PPAR Modulators (4)
  • New PPAR Products
Catalog No. Product Name Information Product Use Citations Product Validations
S2798 GW6471 GW 6471 is a potent antagonist of PPARα with IC50 of 0.24 μM.
J Mol Endocrinol, 2022, JME-21-0239
Cell Rep, 2021, 37(6):109920
Haematologica, 2021, 10.3324/haematol.2021.279770
S2871 T0070907 T0070907 is a potent and selective PPARγ inhibitor with IC50 of 1 nM in a cell-free assay, with a >800-fold selectivity over PPARα and PPARδ. T0070907 significantly decreases the levels of DNA-PKcs and RAD51 proteins in ME-180 and SiHa cells.
Redox Biol, 2022, 50:102256
Front Cell Dev Biol, 2021, 9:745554
J Inflamm Res, 2021, 14:395-411
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.
Int J Pharm, 2019, 570:118661
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.
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.
S7484 FH535 FH535 is a Wnt/β-catenin signaling inhibitor and also a dual PPARγ and PPARδ antagonist.
Sci Rep, 2022, 12(1):7
J Exp Clin Cancer Res, 2021, 40(1):230
Cell Oncol (Dordr), 2021, 10.1007/s13402-021-00590-4
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.
Haematologica, 2021, 10.3324/haematol.2020.267096
Nat Commun, 2019, 10(1):4898
Med Sci Monit, 2018, 24:5914-5924
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
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.
S1729 Gemfibrozil Gemfibrozil (CI-719) is an activator of peroxisome proliferator-activated receptor-alpha (PPARα), used for the treatment of hypercholesterolemia and hypertriglyceridemia.
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
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.
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
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
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.
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.
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.
Haematologica, 2021, 10.3324/haematol.2021.279770
Free Radic Biol Med, 2021, 169:283-293
Aging (Albany NY), 2021, 13(8):11969-11987
S9177 Gypenoside XLIX Gypenoside XLIX, a naturally occurring gynosaponin, is a selective peroxisome proliferator-activated receptor (PPAR)-alpha activator.
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.
S9723 CDDO-Im CDDO-Im (CDDO-Imidazolide, RTA-403, TP-235) 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.
S0531 DG172 dihydrochloride DG-172 dihydrochloride is a novel PPARβ/δ-selective antagonist with the IC50 of 27 nM.
Cell Signal, 2022, 93:110304
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.
Brain Behav Immun, 2022, S0889-1591(22)00025-3
Oxid Med Cell Longev, 2022, 2022:9226022
Front Immunol, 2021, 12:685984
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.
Nat Commun, 2019, 11;10(1):4621
S8025 GSK3787 GSK3787 is as a selective and irreversible antagonist of PPARδ with pIC50 of 6.6, with no measurable affinity for hPPARα or hPPARγ.
J Mol Endocrinol, 2022, JME-21-0239
Cell Death Dis, 2021, 12(3):240
Biol Psychiatry, 2020, S0006-3223(20)31906-5
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.
S1794 Fenofibrate (NSC-281319) Fenofibrate (NSC-281319) 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.
Cell Metab, 2022, 34(2):299-316.e6
Redox Biol, 2021, 46:102082
J Cell Mol Med, 2020, 24(6):3384-3398
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 Cell Mol Med, 2022, 10.1111/jcmm.17154
J Nanobiotechnology, 2021, 19(1):150
S2075 Rosiglitazone (BRL-49653) HCl Rosiglitazone HCl (BRL-49653) is a blood glucose-lowering drugs, stimulating insulin secretion by binding to the PPAR receptors in fat cells.
Cell Death Dis, 2021, 12(11):972
Front Cell Dev Biol, 2021, 9:662868
Antioxidants (Basel), 2021, 10(2)155
S2505 Rosiglitazone (BRL-49653) maleate Rosiglitazone maleate (BRL 49653), 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.
Cell Death Dis, 2021, 12(11):972
Antioxidants (Basel), 2021, 10(2)155
Front Cardiovasc Med, 2021, 8:698056
S2556 Rosiglitazone (BRL 49653) Rosiglitazone (BRL 49653) 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.
Redox Biol, 2022, 50:102256
Toxicology, 2022, 465:153048
Hum Cell, 2022, 10.1007/s13577-022-00671-y
S2590 Pioglitazone (AD-4833) Pioglitazone (AD-4833, U 72107) 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.
Commun Biol, 2022, 5(1):231
J Cell Mol Med, 2022, 10.1111/jcmm.17154
Hum Cell, 2022, 10.1007/s13577-022-00671-y
S2665 Ciprofibrate Ciprofibrate (Win-35833) is a peroxisome proliferator-activated receptor agonist.
Respir Physiol Neurobiol, 2020, 271:103290
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.
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
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.
Clin Exp Reprod Med, 2020, 47(2):108-113
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).
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
S4207 Clofibric Acid Clofibric acid is a PPARα agonist and hypolipidemic agent.
S5615 Cardarine (GW501516) Cardarine (GW501516, Cardarine, GW1516) is a synthetic PPARδ-specific agonist that displays high affinity for PPARδ (Ki=1.1 nM) with > 1000 fold selectivity over PPARα and PPARγ.
Cell Signal, 2022, 93:110304
J Lipid Res, 2014, 55(7):1254-66
S5812 Choline Fenofibrate Choline fenofibrate is a newly developed choline salt of fenofibric acid, a synthetic phenoxy-isobutyric acid derivate with antihyperlipidemic activity that acts as an PPARα agonist.
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
S8432 Troglitazone (CS-045) Troglitazone (Rezulin, Romglizone, Prelay, CS045, Romozin) 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
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
S9199 Pseudoginsenoside F11 Pseudoginsenoside F11, a natural product found in American ginseng but not in Asian ginseng, is a novel partial PPARγ agonist.
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.
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.
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.
Aging (Albany NY), 2019, 11(22):10513-10531
Nature, 2018, 560(7718):372-376
S3868 Harmine Harmine (Telepathine) is an alkaloid of the β-carboline family that regulates PPARγ expression through inhibition of the Wnt signaling pathway. It also selectively binds to MAO-A and reversibly inhibits monoamine oxidase A (MAO-A) but not the variant MAO-B.
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.
S7955 EPI-001 EPI-001 is an androgen receptor N-terminal domain antagonist with IC50 of ∼6 μM and a selective PPAR-gamma modulator.
Prostate, 2019, 79(2):206-214
S2798 GW6471 GW 6471 is a potent antagonist of PPARα with IC50 of 0.24 μM.
J Mol Endocrinol, 2022, JME-21-0239
Cell Rep, 2021, 37(6):109920
Haematologica, 2021, 10.3324/haematol.2021.279770
S2871 T0070907 T0070907 is a potent and selective PPARγ inhibitor with IC50 of 1 nM in a cell-free assay, with a >800-fold selectivity over PPARα and PPARδ. T0070907 significantly decreases the levels of DNA-PKcs and RAD51 proteins in ME-180 and SiHa cells.
Redox Biol, 2022, 50:102256
Front Cell Dev Biol, 2021, 9:745554
J Inflamm Res, 2021, 14:395-411
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.
Int J Pharm, 2019, 570:118661
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.
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.
S7484 FH535 FH535 is a Wnt/β-catenin signaling inhibitor and also a dual PPARγ and PPARδ antagonist.
Sci Rep, 2022, 12(1):7
J Exp Clin Cancer Res, 2021, 40(1):230
Cell Oncol (Dordr), 2021, 10.1007/s13402-021-00590-4
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.
Haematologica, 2021, 10.3324/haematol.2020.267096
Nat Commun, 2019, 10(1):4898
Med Sci Monit, 2018, 24:5914-5924
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
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.
S1729 Gemfibrozil Gemfibrozil (CI-719) is an activator of peroxisome proliferator-activated receptor-alpha (PPARα), used for the treatment of hypercholesterolemia and hypertriglyceridemia.
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
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.
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
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
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.
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.
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.
Haematologica, 2021, 10.3324/haematol.2021.279770
Free Radic Biol Med, 2021, 169:283-293
Aging (Albany NY), 2021, 13(8):11969-11987
S9177 Gypenoside XLIX Gypenoside XLIX, a naturally occurring gynosaponin, is a selective peroxisome proliferator-activated receptor (PPAR)-alpha activator.
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.
S9723 CDDO-Im CDDO-Im (CDDO-Imidazolide, RTA-403, TP-235) 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.
S0531 DG172 dihydrochloride DG-172 dihydrochloride is a novel PPARβ/δ-selective antagonist with the IC50 of 27 nM.
Cell Signal, 2022, 93:110304
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.
Brain Behav Immun, 2022, S0889-1591(22)00025-3
Oxid Med Cell Longev, 2022, 2022:9226022
Front Immunol, 2021, 12:685984
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.
Nat Commun, 2019, 11;10(1):4621
S8025 GSK3787 GSK3787 is as a selective and irreversible antagonist of PPARδ with pIC50 of 6.6, with no measurable affinity for hPPARα or hPPARγ.
J Mol Endocrinol, 2022, JME-21-0239
Cell Death Dis, 2021, 12(3):240
Biol Psychiatry, 2020, S0006-3223(20)31906-5
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.
S1794 Fenofibrate (NSC-281319) Fenofibrate (NSC-281319) 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.
Cell Metab, 2022, 34(2):299-316.e6
Redox Biol, 2021, 46:102082
J Cell Mol Med, 2020, 24(6):3384-3398
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 Cell Mol Med, 2022, 10.1111/jcmm.17154
J Nanobiotechnology, 2021, 19(1):150
S2075 Rosiglitazone (BRL-49653) HCl Rosiglitazone HCl (BRL-49653) is a blood glucose-lowering drugs, stimulating insulin secretion by binding to the PPAR receptors in fat cells.
Cell Death Dis, 2021, 12(11):972
Front Cell Dev Biol, 2021, 9:662868
Antioxidants (Basel), 2021, 10(2)155
S2505 Rosiglitazone (BRL-49653) maleate Rosiglitazone maleate (BRL 49653), 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.
Cell Death Dis, 2021, 12(11):972
Antioxidants (Basel), 2021, 10(2)155
Front Cardiovasc Med, 2021, 8:698056
S2556 Rosiglitazone (BRL 49653) Rosiglitazone (BRL 49653) 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.
Redox Biol, 2022, 50:102256
Toxicology, 2022, 465:153048
Hum Cell, 2022, 10.1007/s13577-022-00671-y
S2590 Pioglitazone (AD-4833) Pioglitazone (AD-4833, U 72107) 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.
Commun Biol, 2022, 5(1):231
J Cell Mol Med, 2022, 10.1111/jcmm.17154
Hum Cell, 2022, 10.1007/s13577-022-00671-y
S2665 Ciprofibrate Ciprofibrate (Win-35833) is a peroxisome proliferator-activated receptor agonist.
Respir Physiol Neurobiol, 2020, 271:103290
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.
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
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.
Clin Exp Reprod Med, 2020, 47(2):108-113
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).
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
S4207 Clofibric Acid Clofibric acid is a PPARα agonist and hypolipidemic agent.
S5615 Cardarine (GW501516) Cardarine (GW501516, Cardarine, GW1516) is a synthetic PPARδ-specific agonist that displays high affinity for PPARδ (Ki=1.1 nM) with > 1000 fold selectivity over PPARα and PPARγ.
Cell Signal, 2022, 93:110304
J Lipid Res, 2014, 55(7):1254-66
S5812 Choline Fenofibrate Choline fenofibrate is a newly developed choline salt of fenofibric acid, a synthetic phenoxy-isobutyric acid derivate with antihyperlipidemic activity that acts as an PPARα agonist.
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
S8432 Troglitazone (CS-045) Troglitazone (Rezulin, Romglizone, Prelay, CS045, Romozin) 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
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
S9199 Pseudoginsenoside F11 Pseudoginsenoside F11, a natural product found in American ginseng but not in Asian ginseng, is a novel partial PPARγ agonist.
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.
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.
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.
Aging (Albany NY), 2019, 11(22):10513-10531
Nature, 2018, 560(7718):372-376
S3868 Harmine Harmine (Telepathine) is an alkaloid of the β-carboline family that regulates PPARγ expression through inhibition of the Wnt signaling pathway. It also selectively binds to MAO-A and reversibly inhibits monoamine oxidase A (MAO-A) but not the variant MAO-B.
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.
S7955 EPI-001 EPI-001 is an androgen receptor N-terminal domain antagonist with IC50 of ∼6 μM and a selective PPAR-gamma modulator.
Prostate, 2019, 79(2):206-214