GW-501516
PPARδ agonist / Potent and selective PPARδ (NR1C2) agonist, EC50=1.2 nM and 1000-fold selective over other PPAR subtypes.1 Induces apolipoprotein A1-mediated cholesterol efflux in vitro.1 Improves hematopoietic stem cell maintenance.2 Prevents downregulation of AMPK caused by a high-fat diet in liver and increases fatty acid oxidation.3 Upregulates human Sirt1 via Sp1 activation.4 Along with exercise, GW-501516 synergistically increases running endurance.5
Biochemicals & reagents
317318-70-0
1) Oliver et al. (2001), A selective peroxisome proliferator-activated receptor delta agonist promotes reverse cholesterol transport; Proc. Natl. Acad. Sci. USA, 98 5306 2) Ito et al. (2012), A PML-PPAR-δ pathway for fatty acid oxidation regulates hematopoietic stem cell maintance; Nat. Med., 18 1350 3) Barroso et al. (2011), The PPARβ/δ activator GW501516 prevents the down-regulation of AMPK caused by a high-fat diet in liver and amplifies the PGC-1α-Lipin 1-PPARα pathway leading to increased fatty acid oxidation. Endocrinology, 152 1848 4) Okazaki et al. (2010), PPAR beta/delta regulates the human SIRT1 gene transcription via Sp1; Endocr. J., 57 403 5) Narkar et al. (2008), AMPK and PPARdelata agonists are exercise mimetics; Cell, 134 405
-20°C
TARGET: Transcription factor -- PATHWAY: Fatty acid metabolism; Cholesterol metabolism; PPAR; Transcription; AMPK pathway -- RESEARCH AREA: Exercise; Stem cells -- DISEASE AREA: Obesity; Liver diseaseDiabetes