PPARα Inhibitors

Common PPARα Inhibitors include, but are not limited to GW6471 CAS 880635-03-0, T0070907 CAS 313516-66-4, GSK 0660 CAS 1014691-61-2, BADGE CAS 1675-54-3 and Sulfasalazine CAS 599-79-1.

Peroxisome proliferator-activated receptors (PPARs) are a group of nuclear receptor proteins that function as transcription factors regulating the expression of genes. These receptors play essential roles in the regulation of cellular differentiation, development, metabolism, and tumorigenesis of higher organisms. Among the PPAR subtypes, PPARα is particularly notable for its influence on lipid metabolism in the liver. When activated, PPARα modulates the transcription of a variety of genes involved in fatty acid oxidation, lipoprotein metabolism, and other metabolic pathways. The activation of PPARα is typically mediated by ligand binding, which induces a conformational change in the receptor, allowing it to form heterodimers with retinoid X receptors (RXRs) and bind to specific DNA sequences known as PPAR response elements (PPREs).

PPARα inhibitors are a class of compounds specifically designed to antagonize the activity of PPARα. These inhibitors work by binding to the ligand-binding domain of the receptor, preventing the conformational changes required for its activation and subsequent gene transcription. By doing so, they effectively reduce or eliminate the transcriptional activity of PPARα.