pparγ coactivator-1α

ZLN005 is an effective and tissue-specific transcriptional activator of PGC-1α.

SR-18292 is an inhibitor of PPAR gamma coactivator-1α (PGC-1α), which increases PGC-1α acetylation, suppresses gluconeogenic gene expression and reduces glucose production in hepatocytes.

RGX-202 (β-GPA) is a creatine analog that alters skeletal muscle energy expenditure. It reduces cellular ATP, creatine, and phosphocreatine levels and stimulates AMP-activated protein kinase (AMPK), activating PPARγ coactivator 1α (PGC-1α).

HD202A is an orally active, selective dual inhibitor of MNK1/MNK2 (with IC50 values of 6.09 nM and 8.06 nM, respectively; Kd values of 1.913 μM and 5.244 μM, respectively), and it inhibits the MNK-eIF4E signaling pathway. By downregulating perilipin 2 and SCD1 while upregulating adipose triglyceride lipase and PPARγ coactivator 1α, HD202A enhances mitochondrial fatty acid oxidation and redox homeostasis. This compound effectively curtails weight gain, hepatic lipid accumulation, and elevated serum lipid levels, while significantly improving glucose tolerance and insulin sensitivity, and reducing inflammatory characteristics. HD202A shows significant potential for research applications in metabolic dysfunction-associated fatty liver disease.

PA-082 is a Novel partial agonist of peroxisome proliferator-activated receptor-γ (PPARγ), recruiting PPARγ-coactivator-1α, preventing triglyceride accumulation, and potentiating insulin signaling in vitro.