BAY-4931 is a potent, covalent and selective PPARγ inverse-agonist with an IC50 of 0.17 nM[1].
Icariin is a flavonol glycoside. Icariin inhibits PDE5 and PDE4 activities with IC50s of 432 nM and 73.50 μM, respectively. Icariin also is a PPARα activator.
GW9578 is a subtype-selective PPARα agonist (EC50s of 5 and 50 nM for murine and human PPAR-α) with potent lipid-lowering activity[1][2].
Ciprofibrate impurity A is an impurity of Ciprofibrate. Ciprofibrate is a PPARα agonist[1].
Wistin, isolated from Caragana sinica roots, is a PPARα and PPARγ agonist[1][2].
Convallatoxin is a cardiac glycoside isolated from Adonis amurensis Regel et Radde. Convallatoxin ameliorates colitic inflammation via activation of PPARγ and suppression of NF-κB. Convallatoxin is a P-glycoprotein (P-gp) substrate and recognized Val982 as an important amino acid involved in its transport. Convallatoxin is an enhancer of ligand-induced MOR endocytosis with high potency and efficacy. Anti-inflammatory and anti-proliferative properties[1][2][3].
PPARγ agonist 4 (Compound 18b) is a potent and selective agonist of PPARγ. PPARγ agonist 4 is not cytotoxic neither on non-resistant nor on resistant cells. PPARγ agonist 4 exerts antitumor potency only in combination with Imatinib[1].
Glycyrin is a PPAR-γ ligand of licorice. Glycyrin can decrease the blood glucose levels of genetically diabetic mice.Glycyrin also shows antibacterial activity[1][2][3].
10-Nitrolinoleic acid is a potent peroxisome proliferator-activated receptor γ (PPARγ) agonist. 10-Nitrolinoleic acid competes with [3H]Rosiglitazone for binding to PPAR-γ, with an IC50 of 0.22 μM[1].
Eicosatetraynoic acid (ETYA) is a nonspecific inhibitor of cyclooxygenase and lipoxygenase (ID50=8 μM and 4 μM, respectively)[1]. Eicosatetraynoic acid (ETYA) activates PPARα and PPARγ chimeras at 10 µM[2].
Norathyriol (Mangiferitin) is a natural metabolite of Mangifera. Norathyriol inhibits α-glucosidase in a noncompetitive manner with an IC50 of 3.12 μM[1]. Norathyriol inhibits PPARα, PPARβ, and PPARγ with IC50s of 92.8 µM, 102.4 µM, and 153.5 µM, respectively[2]. Antioxidant, anticancer, antimicrobial, anti-inflammatory, anti-bacterial activities.
Farglitazar is a PPARγ agonist that has significant therapeutic benefits such as glycemic control in type 2 diabetic patients.
Rosiglitazone (BRL49653) is a potent thiazolidinedione insulin sensitizer. Rosiglitazone is a selective PPARγ agonist with EC50s of 30 nM, 100 nM and 60 nM for PPARγ1, PPARγ2, and PPARγ, respectively.
CAY10410 (11-Oxo-prosta-5Z), a 15d-PGJ2 analog, is a potent PPARγ agonist. CAY10410 has the ability to activate PPARγ in human B cells without killing B lymphocytes[1].
LY518674 is a potent, selective PPARα antagonist, with an EC50 of 42 nM for human PPARα. LY518674 reduces triglycerides in and increased HDL-C and is used for the treatment of atherosclerosis[1][2][3].
ST247 a potent PPARβ/δ inverse agonist. ST247 has a higher affinity to PPARβ/δ. ST247 modulates expression of the activation marker CCL2 in the opposite direction. ST247 efficiently induces the interaction with corepressors. ST247 inhibits the agonist-induced transcriptional activity of PPARβ/δ[1].
Tesaglitazar is a dual peroxisome proliferator-activated receptor (PPAR) alpha/gamma agonist that is more potent on PPARγ than on PPARα, with EC50s of 13.4 μM and 3.6 μM for rat PPARα and human PPARα, respectively, and approximately 0.2 μM for both rat and human PPARγ. Tesaglitazar induces interstitial mesenchymal cell DNA synthesis and fibrosarcomas in subcutaneous tissues in rats[1].
Elafibranor is a PPARα/δ agonist with EC50s of 45 and 175 nM, respectively.
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[1][2].
PPARγ agonist 6 (Compound 12) is a potent and selective agonist of PPARγ. PPARγ agonist 6 has the potential for the research of cancer diseases[1].
Troglitazone-d4 is deuterium labeled Troglitazone. Troglitazone is a PPARγ agonist, with EC50s of 550 nM and 780 nM for human and murine PPARγ receptor, respectively.
Gypenoside XLIX, a dammarane-type glycoside, is a prominent component of G. pentaphyllum. Gypenoside XLIX is a selective peroxisome proliferator-activated receptor (PPAR)-alpha activator and inhibits cytokine-induced vascular cell adhesion molecule-1 (VCAM-1) overexpression and hyperactivity in human endothelial cells[1].
Mesalamine impurity P is an impurity of Mesalamine (HY-15027). 5-Aminosalicylic acid (Mesalamine) acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB[1].
Kihadanin B is a citrus limonoid that can be purified from the peels of immature Citrus unshiu. Kihadanin B suppresses adipogenesis through repression of the Akt-FOXO1-PPARγ axis in 3T3-L1 adipocytes[1].
Darglitazone (CP-86325), a thiazolidinedione, is a potent, selective, and orally active PPAR-γ agonist. Darglitazone is effective in controlling blood glucose and lipid metabolism, and can be used for type II diabetes research[1].
9-cis-Retinoic acid-d5 (ALRT1057-d5) is the deuterium labeled 9-cis-Retinoic acid. 9-cis-Retinoic acid (ALRT1057), a vitamin A derivative, is a potent RAR/RXR agonist. 9-cis-Retinoic acid induces apoptosis, regulates cell cycle and has anticancer, anti-inflammatory and neuroprotection activities[1][2][3][4][5][6].
Fmoc-Ala-OH-13C3 is a 13C-labeled Fmoc-leucine. 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-ind
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[1].
Cinnamyl Alcohol is an active component from chestnut flower, inhibits increased PPARγ expression, with anti-obesity activity[1].
PPARδ agonist 9 (compound 21) is a PPARδ agonist (EC50: 3.6 nM). PPARδ agonist 9 has in vivo efficacy, reducing serum levels of MCP-1 in mice and significantly inhibiting atherosclerosis progression in the LDLr-KO model (inhibition rate: 50-60%)[1].