The peroxisome proliferator-activated receptors (PPARs) α, γ, and δ are ligand-activated transcription factors that play a key role in lipid homeostasis. Activation of PPARα results in increased clearance of triglyceride (TG) rich very low-density lipoprotein (VLDL) via a reduction in plasma levels of ApoCIII and in upregulation of ApoA1, the principal lipoprotein component of HDL.1 GW 590735 is a potent and selective agonist of PPARα with an EC50 value of 4 nM for the expression of a GAL4-responsive reporter gene and at least 500-fold selectivity versus PPARγ and PPARδ.1
1
Sierra, M.L., Beneton, V., Boullay, A., et al. Substituted 2-[(4-aminomethyl)phenoxy]-2-methylpropionic acid PPARα agonists. 1. Discovery of a novel series of potent HDLc raising agents. J Med Chem50685-695(2007).
Sierra, M.L., Beneton, V., Boullay, A., et al. Substituted 2-[(4-aminomethyl)phenoxy]-2-methylpropionic acid PPARα agonists. 1. Discovery of a novel series of potent HDLc raising agents. J Med Chem50685-695(2007).
GW 590735 is available in the following screening
library: