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PPAR
Choose Selective PPAR Inhibitors
PPAR Signaling Pathway Map
Isoform-selective Inhibitors
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. | ||
| 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. |
|
|
| 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. | ||
| 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. |
|
|
| 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. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| 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. |
|
|
| 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. | ||
| 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. |
|
|
| 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. | ||
| 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. |
|
|
| 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. |
|
|
| 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. |
|
|
| 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. |
|
|
| 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. |
|
|
| 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. |
|
|
| 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. |
|
|
| S2665 | Ciprofibrate | Ciprofibrate (Win-35833) is a peroxisome proliferator-activated receptor agonist. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| 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. |
|
|
| 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. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| S2798 | GW6471 | GW 6471 is a potent antagonist of PPARα with IC50 of 0.24 μM. | ||
| 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. |
|
|
| 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. | ||
| 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. |
|
|
| 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. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| 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. |
|
|
| 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. | ||
| 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. |
|
|
| 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. | ||
| 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. |
|
|
| 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. |
|
|
| 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. |
|
|
| 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. |
|
|
| 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. |
|
|
| 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. |
|
|
| 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. |
|
|
| S2665 | Ciprofibrate | Ciprofibrate (Win-35833) is a peroxisome proliferator-activated receptor agonist. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| 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. |
|
|
| 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. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| 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. |
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