WY-14643 | PPARα agonist

WY-14643 (50892-23-4) is a selective PPARα agonist (EC₅₀=0.63, 32 and >100 µM for PPARα,γ and δ, respectively).¹  Displays anti-inflammatory activity² and reduces LPS-induced inflammation in alveolar epithelial cells³. Induces “browning” of white adipocytes in combined treatment with retinoic acid.⁴  Stimulates ADAM10-mediated proteolysis of  amyloid precursor protein in a mouse model.⁵ Down regulates NFkB transcriptional activity. Review.⁶

References/Citations:

1) Forman et al. (1997), Hypolipidemic drugs, polyunsaturated fatty acids and eicosanoids are ligands for peroxisome proliferator-activated receptors alpha and delta; Proc. Natl. Acad. Sci. USA, 94 4312
2) Devchand et al. (1996), The PPARalpha-leukotriene B4 pathway to inflammation control; Nature, 384 39
3) Heckler et al. (2015), PPAR-a activation reduced LPS-induced inflammation in alveolar epithelial cells; Exp. Lung Res., 41 393
4) Wang et al. (2015), WY14643 combined with all-trans retinoic acid acts via p38 MAPK to induce “browning” of white adipocytes in mice; Genet. Mol. Res., 14 6978
5) Corbett et al. (2015), Activation of peroxisome proliferator-activated receptor alpha stimulates ADAM10-mediated proteolysis of APP; Proc. Natl. Acad. Sci. USA, 112 8445
6) Merk et al. (2015), Pirinixic acids: flexible fatty acid mimetics with various biological activities; Future Med. Chem., 7 1597