Signaling Pathway

PPAR

PPAR

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PPARs (Peroxisome proliferator-activated receptors) are ligand-activated transcription factors of nuclear hormone receptor superfamily comprising of the following three subtypes: PPARα, PPARγ, and PPARβ/δ. PPARs play essential roles in the regulation of cellular differentiation, development, and metabolism (carbohydrate, lipid, protein), and tumorigenesis of higher organisms. All PPARs heterodimerize with the retinoid X receptor (RXR) and bind to specific regions on the DNA of target genes. Activation of PPAR-α reduces triglyceride level and is involved in regulation of energy homeostasis. Activation of PPAR-γ causes insulin sensitization and enhances glucose metabolism, whereas activation of PPAR-β/δ enhances fatty acids metabolism.

PPAR Inhibitors & Modulators (40)

Product Name Catalog No. Brief Description
(20S)-Protopanaxatriol

HY-N0835

(20S)-Protopanaxatriol(g-PPT) is a metabolites of ginsenoside, protopanaxatriol (g-PPT), could modulate endothelial cell functions through the glucocorticoid receptor (GR) and oestrogen receptor (ER).

Aleglitazar

HY-14728

Aleglitazar(R1439; RO-0728804) is a new dual PPAR-α/γ agonist with IC50 of 2.8 nM/4.6 nM.

Balaglitazone

HY-16086

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

Bezafibrate

HY-B0637

Bezafibrate(BM15075) is the first clinically tested dual and pan-PPAR co-agonism.

BMS-687453

HY-10678

BMS-687453 is a potent and selective PPARα agonist, with an EC50 of 10 nM for human PPARα and 410-fold selectivity vs human PPARγ in PPAR-GAL4 transactivation assays.

CDDO-Im

HY-15725

CDDO-Im(RTA-403) is a novel synthetic triterpenoid more potent than its parent compound CDDO both in vitro and in vivo; PPARγ agonist.

Choline Fenofibrate

HY-14739

Choline Fenofibrate (ABT-335) is the choline salt of fenofibric acid under clinical development as a combination therapy with rosuvastatin for the management of dyslipidemia.

Ciprofibrate

HY-B0664

Ciprofibrate is a peroxisome proliferator-activated receptor agonist.

Ciprofibrate D6

HY-B0664S

Ciprofibrate D6 is deuterium labeled Ciprofibrate, which is a peroxisome proliferator-activated receptor agonist.

Clofibrate

HY-B0287

Clofibrate (Atromid-S), a fibric acid derivative used in the treatment of hyperlipoproteinemia type III and severe hypertriglyceridemia.

Daidzein

HY-N0019

Daidzein is an inactive analogue of genistein, a tyrosine kinase inhibitor and an estrogen receptor activator.

DG172 dihydrochloride

HY-19737A

DG172 dihydrochloride is a novel PPARβ/δ-selective ligand showing high binding affinity (IC50 = 27 nM) and potent inverse agonistic properties.

Elafibranor

HY-16737

Elafibranor (GFT505) is an agonist of the peroxisome proliferator-activated receptor(PPAR)-α and -δ, induces resolution of nonalcoholic steatohepatitis without fibrosis worsening.

Eupatilin

HY-N0783

Eupatilin, a flavone derived from Artemisia princepsPampanini, has various pharmacological activities, including antioxidant, anti-tumor, and anti-inflammatory capacities.

Fenofibrate

HY-17356

Fenofibrate is PPARα agonist with EC50 of 18 μM and 30 μM for mouse and human PPARα, respectively.

FH535

HY-15721

FH535 is a compound that suppresses both Wnt/beta-catenin and peroxisome proliferator-activated receptor (PPAR) signaling.

Gemfibrozil

HY-B0258

Gemfibrozil (Lopid) is a compound used to lower lipid levels.

GSK0660

HY-12377

GSK0660 is a specific antagonist of PPARβ/δ, also has inverse agonist effects when used alone.

GSK3787

HY-15577

GSK3787 is as a selective and irreversible antagonist of PPARδ with pIC50 of 6.6, with no measurable affinity for hPPARα or hPPARγ.

GW 501516

HY-10838

GW501516(GSK-516; GW1516) is a potent and highly selective PPARβ/δ agonist, with EC50 of 1 nM, with 1000-fold selectivity over hPPARα and hPPARγ.