SR10221 is a potent, selective PPARγ inverse agonist with IC50 of 13 nM in biochemical peptide recruitment assays, represses downstream PPARγ target genes leading to growth inhibition in bladder cancer cell lines.

MMT-160 is a novel selective peroxisome proliferator-activated receptor γ (PPARγ) antagonist with IC50 of 0.17 uM, covalently binds to the PPARγ ligand binding domain (LBD) via Cys285.

MBX-102 acid is the active form of JNJ39659100 (MBX-102), a selective partial PPAR-γ agonist with EC50 of 23.34 uM (hPPAR-γ), enhances insulin sensitivity in vitro in 3T3-L1 adipocytes, binds to the PPAR-γ LBD in a manner that is distinct from but overla

Bocidelpar is a modulator of peroxisome proliferator-activated receptor delta (PPAR-δ). Bocidelpar improves mitochondrial biogenesis and function in Duchenne Muscular Dystrophy (DMD) muscle cells (extracted from patent WO2017062468A1, compound 2b).

GW501516 is the most selective and potent PPARβ (EC50=1.1nM) agonist that has been demonstrated to be 1,000-fold more selective in comparison to existing subtypes.

WY 14643 (Pirinixic Acid) is a potent peroxisome proliferator and activator of PPARα with ED50 of 1.5 μM.

Rosiglitazone maleate is a potent and selective activator of PPARγ, with EC50s of 30 nM, 100 nM and 60 nM for PPARγ1, PPARγ2, and PPARγ, respectively, and a Kd of appr 40 nM for PPARγ; Rosiglitazone maleate is also an modulator of TRP channels, inhibits T

T0070907 is a potent and selective PPARγ antagonist with IC50 of 1 nM; displays > 800-fold selectivity for PPARγ over PPARα and PPARδ.

Pioglitazone Hydrochloride is the hydrochloride salt preparation of Pioglitazone, a specific ligand of PPAR-γ (peroxisome proliferator-activated receptor-γ). Pioglitazone is a thiazolidinedione compound described to produce antiinflammatory and antiarteri

Pemafibrate is an orally bioavailable and selective agonist of peroxisome proliferator-activated receptor α (PPARα; EC50 = 1 nM for transcriptional activity), a transcription factor that is essential for regulation of lipid homeostasis.

GW9662 is a selective PPAR antagonist, inhibiting PPARγ, PPARα and PPARδ with IC50 of 3.3 nM, 32 nM and 2 μM, respectively.

GSK3787 is as a potent and selective antagonist of PPARδ with pIC50 of 6.6.

GSK-0660 is a selective PPARδ antagonist (IC50 values are 0.155, > 10 and ≥ 10 μM at PPARδ, PPARα and PPARγ respectively).

Balaglitazone (DRF-2593; NN-2344) is a novel partial agonist of PPAR-γ.

BMS687453 is a potent and selective peroxisome proliferator activated receptor (PPAR) α agonist, with an EC50 of 10 nM for human PPARα and ∼410-fold selectivity vs human PPARγ in PPAR-GAL4 transactivation assays.

A PPARα agonist and an irreversible CPT-1 inhibitor.

Mesalamine impurity P is an impurity of Mesalamine. 5-Aminosalicylic acid (Mesalamine) acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB.

Rosiglitazone (BRL 49653) potassium is an orally active selective PPARγ agonist (EC50: 60 nM, Kd: 40 nM). Rosiglitazone potassium is a TRPC5 activator (EC50: 30 μM) and TRPM3 inhibitor. Rosiglitazone potassium can be used in the research of obesity and diabetes, senescence, ovarian cancer.

Pioglitazone (U 72107) potassium is an orally active and selective PPARγ (peroxisome proliferator-activated receptor) agonist with high affinity binding to the PPARγ ligand-binding domain with EC50 of 0.93 μM and 0.99 μM for human and mouse PPARγ, respectively. Pioglitazone potassium can be used in diabetes research.

GW1929 hydrochloride is an orally active peroxisome proliferator-activated receptor-γ (PPARγ) agonist with a pKi of 8.84 for human PPAR-γ, and pEC50s of 8.56 and 8.27 for human PPAR-γ and murine PPAR-γ, respectively. GW1929 hydrochloride has antidiabetic efficacy and neuroprotective potential. GW1929 hydrochloride suppresses neuronal apoptosis and shows anti-inflammatory potential.

2-Tetradecylthio acetic acid is a pan-peroxisome proliferator activated receptor (pan-PPAR) activator. 2-Tetradecylthio acetic acid induces hypolipidemia. 2-Tetradecylthio acetic acid reduces plasma lipids and enhances hepatic fatty acid oxidation in rodents. 2-Tetradecylthio acetic acid increases the expression of genes involved in fatty acid uptake, activation, accumulation, and oxidation.

Leriglitazone (Hydroxypioglitazone) hydrochloride, a metabolite of pioglitazone. Leriglitazone (Hydroxypioglitazone) hydrochloride PioOH is a PPARγ agonist, stabilizes the PPARγ activation function-2 (AF-2) co-activator binding surface and enhances co-activator binding, affording slightly better transcriptional efficacy. Leriglitazone (Hydroxypioglitazone) hydrochloride binds to the PPARγ C-terminal ligand-binding domain (LBD) with a Ki of 1.2 μM，Leriglitazone induces transcriptional efficacy of the PPARγ (LBD) with an EC50 of 680 nM.

H-​Trp-​Glu-​OH is a selective, reversible and cell-permeable PPARγ with a Kd of ~8 µM. H-​Trp-​Glu-​OH might be developed as a possible lead compound in diabetes research.

Fmoc-leucine is a selective PPARγ modulator. Fmoc-leucine activates PPARγ with a lower potency but a similar maximal efficacy than rosiglitazone. Fmoc-leucine improves insulin sensitivity in normal, diet-induced glucose-intolerant, and in diabetic db/db mice. Fmoc-leucine has a lower adipogenic activity.

S26948 is a specific peroxisome proliferator-activated receptor γ (PPARγ) modulator (EC50=8.83 nM) with potent antidiabetes and antiatherogenic effects. S26948 is a specific high-affinity agonist for PPARγ.

WO95E is a novel potent, synthetic ligand (partial agonist) of PPARγ, directly binds to PPARγ with IC50 of 11 nM; WO95E's binding affinity is approximately 70-fold lower than that of UHC1 (Journal of Biological Chemistry. 2014;289(38):26618–26629.). WO95E significantly inhibited the S273 phosphorylation of PPARγ in 3T3-L1 differentiated adipocytes, led to the upregulation of the mRNA levels of a number of the PPARγ phosphorylation-dependent genes, including adiponectin, cycp2f2, Ddx-17, Rarres2, and Selenbp1. Unlike SR1664 and UHC1, WO95E does not bind to the canonical PPARγ ligand-binding pocket (LBP) containing H3, H3-4 loop, H11 and H12, which full agonist Rosi binds, instead, WO95E binds to the ABP comprising H2′-H3, β-sheet, and the Ω loop. WO95E improved glucose tolerance and insulin sensitivity in DIO mice.

PPARγ pSer273-IN-10 is a specific, in vivo-active small molecule inhibitor of CDK5-mediated Ser273 phosphorylation of PPARγ without classical PPARγ agonism.PPARγ pSer273-IN-10 is a potent PPARγ binder and in vitro inhibitor of the CDK5-mediated phosphorylation of PPARγ Ser273 and displays negligible PPARγ agonism in a reporter gene assay. PPARγ pSer273-IN-10 demonstrated an improvement in insulin sensitivity in the ob/ob diabetic mouse model in 7 day treatment in vivo testing.

NXT629 (NXT-629) is a potent, selective PPARα antagonist with IC50 of 77 nM (human PPARα), no effect against PPARδ and PPARγ (IC50>30 uM).NXT629 inhibited agonist-induced transcription of PPARα-regulated genes, demonstrating target engagement in chronic lymphocytic leukemia (CLL) cells.NXT629 induced apoptosis of CLL cells even in the presence of a protective microenvironment.NXT629 reduces the number of chronic leukemia cells undergoing cell division with IC50 of 9.6 uM.NXT629 reduces CLL tumor burden delays disease progression of CLL in CLL mouse model.

PPARα/δ agonist 1 is a potent PPARα/PPARδ dual agonist (PPARα EC50=7.0 nM; PPARδ EC50=8.4 nM). PPARα/δ agonist 1 is a high selectivity over PPARγ (PPARγ EC50=1316.1 nM). PPARα/δ agonist 1 has the potential for the research of nonalcoholic steatohepatitis.

SR2595 is an inverse agonist of PPARγ with an IC50 of 30 nM.