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PPAR Agonists

Cat.No. Product Name Information Product Use Citations Product Validations
S2556 Rosiglitazone (BRL 49653) 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.
Signal Transduct Target Ther, 2025, 10(1):394
Nat Commun, 2025, 16(1):6241
Lab Invest, 2025, 105(4):104103
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S2590 Pioglitazone (U-72107) 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.
Front Pharmacol, 2025, 16:1559446
Signal Transduct Target Ther, 2024, 9(1):257
Cell Commun Signal, 2024, 22(1):266
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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. This compound also modulates TRP channels and induces autophagy. It prevents ferroptosis.
Stem Cell Reports, 2022, 17(11):2531-2547
Cell Death Dis, 2021, 12(11):972
Antioxidants (Basel), 2021, 10(2)155
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S2075 Rosiglitazone HCl Rosiglitazone HCl is a blood glucose-lowering drugs, stimulating insulin secretion by binding to the PPAR receptors in fat cells.
J Immunother Cancer, 2024, 12(11)e009805
Stem Cell Reports, 2022, 17(11):2531-2547
Cell Death Dis, 2021, 12(11):972
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S1794 Fenofibrate Fenofibrate is a compound of the fibrate class and fibric acid derivative. This compound is a selective agonist of PPARα with EC50 of 30 μM. It 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. This chemical induces autophagy.
J Cell Mol Med, 2025, 29(7):e70524
J Immunother Cancer, 2024, 12(11)e009805
Heliyon, 2024, 10(11):e31861
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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.
Cell Commun Signal, 2024, 22(1):266
Med Oncol, 2024, 41(8):188
Life Sci, 2021, 279:119696
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S8432 Troglitazone (CS-045) 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.
CNS Neurosci Ther, 2024, 30(8):e14911
Int J Mol Med, 2024, 53(4)37
Free Radic Biol Med, 2021, 163:234-242
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. This compound, 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
S4159 Bezafibrate Bezafibrate (BM 15075) is the first clinically tested dual and pan-PPAR co-agonism.
BMC Cancer, 2025, 25(1):1404
Nat Commun, 2021, 12(1):1929
PPAR Res, 2021, 2021:5589342
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.
Cell Commun Signal, 2025, 23(1):206
Biomed Pharmacother, 2025, 191:118406
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.
Biochem Pharmacol, 2025, 241:117171
Life Sci, 2021, S0024-3205(20)31752-5
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.
Apoptosis, 2025, 10.1007/s10495-025-02193-y
Front Pharmacol, 2024, 15:1488367
S1473 GW501516 (GSK-516, Cardarine) GW501516 is a potent and highly selective PPARβ/δ agonist, with EC50 of 1 nM, with 1000-fold selectivity over hPPARα and hPPARγ. Phase 4.
Adv Ther-Germany, 2023, 6, 2300141
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
E2876 pemafibrate Pemafibrate(K-877) is a selective agonist of peroxisome proliferator-activated receptor (PPAR) α with an IC50 of 10 µM.
Nat Commun, 2025, 16(1):1237
S3720 Elafibranor Elafibranor (GFT505) is an agonist of the peroxisome proliferator-activated receptor-α(PPAR-alpha) and peroxisome proliferator-activated receptor-δ(PPAR-δ). This compound 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.
S6635 Seladelpar Seladelpar(MBX-8025) is a potent and selective agonist of peroxisome proliferator–activated receptor-delta (PPAR-δ) with EC50 of 2 nM for human PPAR-δ. MBX-8025 enhances insulin sensitivity, counters dyslipidemia, and reduces hepatic storage of lipotoxic lipids, thereby ameliorating NASH pathology in obese diabetic mice.
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.
E5858New Chiglitazar (Carfloglitazar) Chiglitazar (Carfloglitazar) is a potent dual agonist of PPARα and PPARγ with EC50 values of 1.2 μM and 0.08 μM, respectively, and also activates PPARδ with an EC50 of 1.7 μM. It effectively improves insulin resistance and corrects dyslipidemia in monosodium L-glutamate (MSG)-induced obese rats.
E1699 SR10221 SR10221 is a inverse-agonist of PPARγ with IC50 of 1.6 nM in RT112/84 FABP4-NLucP reporter assay. It exhibits an antiproliferative activity in vitro.
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.
E7397 (+)-Falcarindiol Falcarindiol is a cytotoxic and anti-inflammatory polyacetylenic oxylipin found in food plants of the Apiaceae family, such as carrots. It functions as a partial agonist of peroxisome proliferator-activated receptor γ (PPARγ) with an EC50 of 3.29 µM in a luciferase reporter assay, leading to the upregulation of the cholesterol transporter ABCA1 in cells. It also promotes a beige adipocyte-like phenotype and enhances mitochondrial respiration in human preadipocyte-derived adipocytes.
E1775 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.
S8027New GW1929 GW1929 is a potent and selective agonist of PPARγ with a pKi of 8.84 for human PPARγ and pEC50 of 8.56 and 8.27 in human and murine receptors, respectively. It exhibits potential clinical benefits in managing diabetic dyslipidemias and cardiovascular risk factors through its lipid-lowering effects and improved insulin sensitivity mediated by PPARγ activation.
E1831 FX-909 FX-909 is an orally available inverse agonist and inhibitor of the transcription factor (TF) peroxisome proliferator activated receptor gamma (PPARG, PPARγ) ), which exhibits anti-tumor activity in vivo.
S2046 Pioglitazone HCl Pioglitazone HCl (AD-4833, U-72107E) is an inhibitor of cytochrome P450 (CYP)2C8 and CYP3A4 enzymes. This compound inhibits CYP2C8, CYP3A4 and CYP2C9 with Ki of 1.7 μM, 11.8 μM and 32.1 μM, respectively. It 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. This chemical inhibits mitochondrial iron uptake, lipid peroxidation, and subsequent ferroptosis.
J Transl Med, 2024, 22(1):593
Commun Biol, 2022, 5(1):231
J Genet Genomics, 2022, S1673-8527(22)00133-3
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