PPAR Agonists
| Cat.No. | Product Name | Information | Product Use Citations | Product Validations |
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| S2556 | Rosiglitazone (BRL 49653) | Rosiglitazone is a potent antihyperglycaemic agent and a potent thiazolidinedione insulin sensitiser 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. |
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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. |
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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. |
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| S2075 | Rosiglitazone HCl | Rosiglitazone HCl is a blood glucose-lowering drug, stimulating insulin secretion by binding to the PPAR receptors in fat cells. |
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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. |
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| S8020 | GW0742 | GW0742 is a potent and highly selective PPARβ/ l delta agonist, with IC50 of 1 nM, with 1000-fold selectivity over hPPAR lpha and hPPAR lgamma. |
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| S8432 | Troglitazone (CS-045) | Troglitazone is a potent agonist for the peroxisome proliferator-activated receptor-(PPAR), which 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. |
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| S3846 | Eupatilin | Eupatilin (NSC 122413), a major flavonoid from Artemisia plants, possesses various beneficial biological effects including anti-inflammation, anti-tumour, 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. |
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| S4159 | Bezafibrate | Bezafibrate (BM 15075) is the first clinically tested dual and pan-PPAR co-agonism. |
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| 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. |
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| 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. |
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| 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. |
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| 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. |
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| S2665 | Ciprofibrate | Ciprofibrate (Win-35833) is a peroxisome proliferator-activated receptor agonist. |
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| S4207 | Clofibric Acid | Clofibric Acid (Chlorofibrinic acid) is a PPARα agonist and hypolipidaemic agent. |
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| E2876 | pemafibrate | Pemafibrate (K-877) is a selective agonist of peroxisome proliferator-activated receptor (PPAR) α with an IC50 of 10 µM. |
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| 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. |
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| 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 dyslipidaemia, 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 an inverse-agonist of PPARγ with an IC50 of 1.6 nM in the RT112/84 FABP4-NLucP reporter assay. It exhibits 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 sensitiser, 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-tumour 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 (PPAR l r ) agonist with EC50 of 0.93 μM and 0.99 μM for human PPAR l r and mouse PPAR l r , respectively. This chemical inhibits mitochondrial iron uptake, lipid peroxidation, and subsequent ferroptosis. |
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