PPAR

Signaling Pathway Map

Research Area

Inhibitory Selectivity

Isoform-specific Inhibitors

PPAR Products

Catalog No.	Information	Product Use Citations	Product Validations
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.	Cancer Lett, 2020, 476:34-47 Front Immunol, 2020, 11:1224 Int J Mol Sci, 2020, 27;21(5):1615	Knocking down LKB1 reversed the PPARc antagonist T0070907-induced changes in the protein expression of the M1 markers (iNOS, green) and the M2 markers (CD206, red) by immunofluorescence staining. Scale bar = 20 μm.
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, 2019, 10(1):4898
S2798	GW6471 GW6471 is an inhibitor of PPARα with IC50 of 0.24 μM.
S7484	FH535 FH535 is a Wnt/β-catenin signaling inhibitor and also a dual PPARγ and PPARδ antagonist.	Gastroenterology, 2019, 10.1053/j.gastro.2019.11.013 J Endocr Soc, 2019, 3(7):1246-1260 Gene, 2019, 684:95-103	Ki-67 staining in xenograft tissues from FH535-treated and control group. Magnifications: ×200 in left column, ×400 in right column.
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 is an antioxidant used in foods especially animal fats and vegetable oils, also in a wide variety of cosmetics and beauty care products.
S4527	Fenofibric acid Fenofibric acid is a fibrate that acts as a lipid-lowering agent, decreasing low-density lipoprotein cholesterol and triglycerides.	Int J Pharm, 2019, 570:118661
S9129	20(S)-Ginsenoside Rh1 20(S)-Ginsenoside 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.
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.
S8029	WY-14643 (Pirinixic Acid) WY 14643 (Pirinixic Acid, NSC 310038) is a potent peroxisome proliferator and activator of PPARα with EC50 of 1.5 μM.	Genes Dev, 2020, 34(7-8):526-543 Environ Pollut, 2020, 29;264:114659 Biomed Pharmacother, 2020, 127:110155	(A) Acot1 mRNA following adenovirus treatments and 0.1% Wy-14643 supplementation (n=7-9). (B) H&E staining shows that Wy-14643 reduced and normalized lipid droplet accumulation in the Acot1 knockdown treatment group.
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
S9189	Oroxin A Oroxin A, an active component isolated from the herb Oroxylum indicum (L.) Kurz, activates PPARγ and inhibits α-glucosidase, exerting antioxidant activity.
S5121	Phytol 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.
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.
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.
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.	J Steroid Biochem Mol Biol, 2019, 10.1016/j.jsbmb.2018.07.005
S9177	Gypenoside XLIX Gypenoside XLIX, a naturally occurring gynosaponin, is a selective peroxisome proliferator-activated receptor (PPAR)-alpha activator.
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 Exp Clin Cancer Res, 2020, 39(1):24 Signal Transduct Target Ther, 2020, 4;5(1):20 Biomed Pharmacother, 2020, 129:110356	Primary microglia (G) were pretreated with JuA at indicated concentrations with or without GW9662 (2 μM) for 18 h, and then incubated with 2 mg/mL Aβ42 in the presence of vehicle (DMSO) or drug for an additional 24 h. The intracellular Aβ42 levels were measured using ELISA.
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.	Theranostics, 2019, 9(12):3501-3514 Nat Med, 2018, 24(3):360-367 Neuropharmacology, 2017, 113(Pt A):396-406	PPARβ/δ activation protects against corticosterone-induced astrocyte damage. (a) Astrocytes treated with Cort at concentrations of 1, 10, and 100 μM( n = 4; F = 329.412 > F0.01 (3, 12); P < 0.01 vs. Con group); (b) MTT assay performed 24 hours after treatment with Cort (10 μM) and GW (0.1, 1, and 10 μM) (n = 5; F = 7.402 > F 0.01 (4, 20); P < 0.01 vs. Con group; #P < 0.05 vs. Cort. group); (c) MTT assay performed after 24 hours of treatment with Cort (10 μM), GW (10 μM), and GSK (10 μM) (n = 4; F = 42.431 > F0.01 (3, 12); P < 0.01 vs. Con group; ##P < 0.01 vs. Cort group; ††P < 0.01 vs. GW group); (d) MTT assay performed 24 hours after treatment with GSK (0.1, 1, and 10 μM) (n = 4; F = 1.659 < F0.01 (3, 12); P > 0.05 vs. Con group); (e) PPARβ/δ expression levels measured by RT-qPCR (n = 4; F = 27.018 > F0.01 (3, 12); P < 0.01 vs. Con group; #P < 0.05 vs. Cort group; †P < 0.05 vs. GW group); (f) PPARβ/δ expression levels measured by Western blot (n = 4; F = 34.723 > F0.01 (3, 12); **P < 0.01vs. Con group; ##P < 0.01 vs. Cort group; †P < 0.05 vs. GW group). Groups were compared using 1-way ANOVA with post hoc Tukey’s multiple comparisons test. Each data point represents the mean ± SEM. Con, Control; Cort, Corticosterone; GW, GW0742; GSK, GSK3787.
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
S2505	Rosiglitazone 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.	Virol Sin, 2019, 34(6):648-661 Drugs R D, 2017, 10.1007/s40268-016-0166-4 J Inflamm (Lond), 2016, 13:19	Total and phosphorylated Akt were detected by western blot in protein lysates of liver, inguinal WAT and gastrocnemius muscle from mice that were treated with an insulin bolus after an overnight fast.
S2556	Rosiglitazone 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.	Nat Commun, 2020, 11(1):71 Cancer Cell Int, 2020, 19;20:58 Cancer Chemother Pharmacol, 2020, 85(2):273-284
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.	Cancer Lett, 2020, 476:34-47 Front Immunol, 2020, 11:1224 FEBS J, 2020, 287(3):529-545	PPARγ activation, but not PPARα activation, increases β-klotho expression and FGF21 signaling. Protein (A) levels of β-klotho in hepatocytes after stimulation with or without 20μM Wy14643/Pioglitazone/Rosiglitazone for 24h
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.	Cells, 2019, 8(12) Int J Med Sci, 2019, 16(12):1593-1603 Sci Rep, 2017, 7:45234	(b) Western blotting used to analyze the expression of caspase-12. The caspase-12 levels were quantified and normalized to the GAPDH levels (n=6; F=23.785>F0.01(3, 20); ∗∗P < 0.01 vs. Con group; ##P < 0.01 vs. Cort group; ††P < 0.01 vs. GW group); (c) Western blotting used to analyze the ratio of cleaved caspase-3 to caspase-3 of the different groups (n=4; F=10.419>F0.01(3, 12); ∗∗P < 0.01 vs. Con group; #P < 0.05 vs. Cort group; †P < 0.05 vs. GW group). Groups were compared using 1-way ANOVA with post hoc Tukey's multiple comparisons test. The data are presented as the mean ± SEM. Con, Control; Cort, Corticosterone; GW, GW0742; GSK, GSK3787
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.	Biol Pharm Bull, 2019, 42(8):1303-1309 Mol Nutr Food Res, 2017, 10.1002/mnfr.201601075 Drug Metab Dispos, 2013, 42(3):318-22	Primary hepatocytes were treated with or without 20μM Wy14643/Pioglitazone/Rosiglitazone for 24h followed by stimulation with or without 1μg/ml recombinant human FGF21 for 15min. FGF21 signaling was analyzed by phosphorylation of ERK1/2 and FRS2 examination.
S2665	Ciprofibrate Ciprofibrate is a peroxisome proliferator-activated receptor agonist.	Respir Physiol Neurobiol, 2020, 271:103290
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.
S1794	Fenofibrate Fenofibrate (Tricor, Trilipix) 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.	J Cell Mol Med, 2020, 24(6):3384-3398 Cancer Discov, 2020, CD-20-0160 Int J Biol Macromol, 2019, 134:759-769	E. The mTOR-lipin1-SREBP1 pathway in the liver of the Rab8af/f and Rab8a-mKO female mice gavaged with fenofibrate (25 mg/kg) or vehicle (H2O) for 8 days. F. mRNA expression of key genes in lipid metabolism in the liver of the Rab8af/f and Rab8a-mKO female mice gavaged with fenofibrate or vehicle for 8 days. n = 4-6. Statistical analyses were carried out using two-way ANOVA. * indicates p <0.05. n.s., not significant.
S2075	Rosiglitazone HCl Rosiglitazone HCl is a blood glucose-lowering drugs, stimulating insulin secretion by binding to the PPAR receptors in fat cells.	Reprod Toxicol, 2016, 61:162-8 Toxicol Appl Pharmacol, 2015, 285(1):51-60 J Leukoc Biol, 2014, 95(4):587-98
S9199	Pseudoginsenoside F11 Pseudoginsenoside F11, a natural product found in American ginseng but not in Asian ginseng, is a novel partial PPARγ agonist.
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.
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
S3786	Glabridin Glabridin, 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.
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.	Nat Commun, 2019, 11;10(1):4621
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).
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.
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.
S9480	Raspberry Ketone Raspberry ketone 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.
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.
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
S3834	Astaxanthin 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 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

Catalog No.	Information	Product Use Citations	Product Validations
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.	Cancer Lett, 2020, 476:34-47 Front Immunol, 2020, 11:1224 Int J Mol Sci, 2020, 27;21(5):1615	Knocking down LKB1 reversed the PPARc antagonist T0070907-induced changes in the protein expression of the M1 markers (iNOS, green) and the M2 markers (CD206, red) by immunofluorescence staining. Scale bar = 20 μm.
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, 2019, 10(1):4898
S2798	GW6471 GW6471 is an inhibitor of PPARα with IC50 of 0.24 μM.
S7484	FH535 FH535 is a Wnt/β-catenin signaling inhibitor and also a dual PPARγ and PPARδ antagonist.	Gastroenterology, 2019, 10.1053/j.gastro.2019.11.013 J Endocr Soc, 2019, 3(7):1246-1260 Gene, 2019, 684:95-103	Ki-67 staining in xenograft tissues from FH535-treated and control group. Magnifications: ×200 in left column, ×400 in right column.
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 is an antioxidant used in foods especially animal fats and vegetable oils, also in a wide variety of cosmetics and beauty care products.
S4527	Fenofibric acid Fenofibric acid is a fibrate that acts as a lipid-lowering agent, decreasing low-density lipoprotein cholesterol and triglycerides.	Int J Pharm, 2019, 570:118661
S9129	20(S)-Ginsenoside Rh1 20(S)-Ginsenoside 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.
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.

Catalog No.	Information	Product Use Citations	Product Validations
S8029	WY-14643 (Pirinixic Acid) WY 14643 (Pirinixic Acid, NSC 310038) is a potent peroxisome proliferator and activator of PPARα with EC50 of 1.5 μM.	Genes Dev, 2020, 34(7-8):526-543 Environ Pollut, 2020, 29;264:114659 Biomed Pharmacother, 2020, 127:110155	(A) Acot1 mRNA following adenovirus treatments and 0.1% Wy-14643 supplementation (n=7-9). (B) H&E staining shows that Wy-14643 reduced and normalized lipid droplet accumulation in the Acot1 knockdown treatment group.
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
S9189	Oroxin A Oroxin A, an active component isolated from the herb Oroxylum indicum (L.) Kurz, activates PPARγ and inhibits α-glucosidase, exerting antioxidant activity.
S5121	Phytol 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.
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.
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.
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.	J Steroid Biochem Mol Biol, 2019, 10.1016/j.jsbmb.2018.07.005
S9177	Gypenoside XLIX Gypenoside XLIX, a naturally occurring gynosaponin, is a selective peroxisome proliferator-activated receptor (PPAR)-alpha activator.

Catalog No.	Information	Product Use Citations	Product Validations
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 Exp Clin Cancer Res, 2020, 39(1):24 Signal Transduct Target Ther, 2020, 4;5(1):20 Biomed Pharmacother, 2020, 129:110356	Primary microglia (G) were pretreated with JuA at indicated concentrations with or without GW9662 (2 μM) for 18 h, and then incubated with 2 mg/mL Aβ42 in the presence of vehicle (DMSO) or drug for an additional 24 h. The intracellular Aβ42 levels were measured using ELISA.
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.	Theranostics, 2019, 9(12):3501-3514 Nat Med, 2018, 24(3):360-367 Neuropharmacology, 2017, 113(Pt A):396-406	PPARβ/δ activation protects against corticosterone-induced astrocyte damage. (a) Astrocytes treated with Cort at concentrations of 1, 10, and 100 μM( n = 4; F = 329.412 > F0.01 (3, 12); P < 0.01 vs. Con group); (b) MTT assay performed 24 hours after treatment with Cort (10 μM) and GW (0.1, 1, and 10 μM) (n = 5; F = 7.402 > F 0.01 (4, 20); P < 0.01 vs. Con group; #P < 0.05 vs. Cort. group); (c) MTT assay performed after 24 hours of treatment with Cort (10 μM), GW (10 μM), and GSK (10 μM) (n = 4; F = 42.431 > F0.01 (3, 12); P < 0.01 vs. Con group; ##P < 0.01 vs. Cort group; ††P < 0.01 vs. GW group); (d) MTT assay performed 24 hours after treatment with GSK (0.1, 1, and 10 μM) (n = 4; F = 1.659 < F0.01 (3, 12); P > 0.05 vs. Con group); (e) PPARβ/δ expression levels measured by RT-qPCR (n = 4; F = 27.018 > F0.01 (3, 12); P < 0.01 vs. Con group; #P < 0.05 vs. Cort group; †P < 0.05 vs. GW group); (f) PPARβ/δ expression levels measured by Western blot (n = 4; F = 34.723 > F0.01 (3, 12); **P < 0.01vs. Con group; ##P < 0.01 vs. Cort group; †P < 0.05 vs. GW group). Groups were compared using 1-way ANOVA with post hoc Tukey’s multiple comparisons test. Each data point represents the mean ± SEM. Con, Control; Cort, Corticosterone; GW, GW0742; GSK, GSK3787.
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

Catalog No.

Information

Product Use Citations

Product Validations

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 Exp Clin Cancer Res, 2020, 39(1):24

Signal Transduct Target Ther, 2020, 4;5(1):20

Biomed Pharmacother, 2020, 129:110356

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.

Theranostics, 2019, 9(12):3501-3514

Nat Med, 2018, 24(3):360-367

Neuropharmacology, 2017, 113(Pt A):396-406

S5817

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

Catalog No.	Information	Product Use Citations	Product Validations
S2505	Rosiglitazone 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.	Virol Sin, 2019, 34(6):648-661 Drugs R D, 2017, 10.1007/s40268-016-0166-4 J Inflamm (Lond), 2016, 13:19	Total and phosphorylated Akt were detected by western blot in protein lysates of liver, inguinal WAT and gastrocnemius muscle from mice that were treated with an insulin bolus after an overnight fast.
S2556	Rosiglitazone 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.	Nat Commun, 2020, 11(1):71 Cancer Cell Int, 2020, 19;20:58 Cancer Chemother Pharmacol, 2020, 85(2):273-284
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.	Cancer Lett, 2020, 476:34-47 Front Immunol, 2020, 11:1224 FEBS J, 2020, 287(3):529-545	PPARγ activation, but not PPARα activation, increases β-klotho expression and FGF21 signaling. Protein (A) levels of β-klotho in hepatocytes after stimulation with or without 20μM Wy14643/Pioglitazone/Rosiglitazone for 24h
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.	Cells, 2019, 8(12) Int J Med Sci, 2019, 16(12):1593-1603 Sci Rep, 2017, 7:45234	(b) Western blotting used to analyze the expression of caspase-12. The caspase-12 levels were quantified and normalized to the GAPDH levels (n=6; F=23.785>F0.01(3, 20); ∗∗P < 0.01 vs. Con group; ##P < 0.01 vs. Cort group; ††P < 0.01 vs. GW group); (c) Western blotting used to analyze the ratio of cleaved caspase-3 to caspase-3 of the different groups (n=4; F=10.419>F0.01(3, 12); ∗∗P < 0.01 vs. Con group; #P < 0.05 vs. Cort group; †P < 0.05 vs. GW group). Groups were compared using 1-way ANOVA with post hoc Tukey's multiple comparisons test. The data are presented as the mean ± SEM. Con, Control; Cort, Corticosterone; GW, GW0742; GSK, GSK3787
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.	Biol Pharm Bull, 2019, 42(8):1303-1309 Mol Nutr Food Res, 2017, 10.1002/mnfr.201601075 Drug Metab Dispos, 2013, 42(3):318-22	Primary hepatocytes were treated with or without 20μM Wy14643/Pioglitazone/Rosiglitazone for 24h followed by stimulation with or without 1μg/ml recombinant human FGF21 for 15min. FGF21 signaling was analyzed by phosphorylation of ERK1/2 and FRS2 examination.
S2665	Ciprofibrate Ciprofibrate is a peroxisome proliferator-activated receptor agonist.	Respir Physiol Neurobiol, 2020, 271:103290
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.
S1794	Fenofibrate Fenofibrate (Tricor, Trilipix) 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.	J Cell Mol Med, 2020, 24(6):3384-3398 Cancer Discov, 2020, CD-20-0160 Int J Biol Macromol, 2019, 134:759-769	E. The mTOR-lipin1-SREBP1 pathway in the liver of the Rab8af/f and Rab8a-mKO female mice gavaged with fenofibrate (25 mg/kg) or vehicle (H2O) for 8 days. F. mRNA expression of key genes in lipid metabolism in the liver of the Rab8af/f and Rab8a-mKO female mice gavaged with fenofibrate or vehicle for 8 days. n = 4-6. Statistical analyses were carried out using two-way ANOVA. * indicates p <0.05. n.s., not significant.
S2075	Rosiglitazone HCl Rosiglitazone HCl is a blood glucose-lowering drugs, stimulating insulin secretion by binding to the PPAR receptors in fat cells.	Reprod Toxicol, 2016, 61:162-8 Toxicol Appl Pharmacol, 2015, 285(1):51-60 J Leukoc Biol, 2014, 95(4):587-98
S9199	Pseudoginsenoside F11 Pseudoginsenoside F11, a natural product found in American ginseng but not in Asian ginseng, is a novel partial PPARγ agonist.
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.
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
S3786	Glabridin Glabridin, 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.
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.	Nat Commun, 2019, 11;10(1):4621
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).
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.
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.
S9480	Raspberry Ketone Raspberry ketone 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.
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.

Catalog No.	Information	Product Use Citations
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
S3834	Astaxanthin 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 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

Catalog No.

Information

Product Use Citations

Product Validations

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

S3834

Astaxanthin

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 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