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Soluble in DMSO. GW590735 is a potent and selective PPARalpha agonist. It stimulated PPARalpha with an EC50 of 4 nM and had at least 500-fold selectivity on PPARalpha versus PPARdelta and PPARgamma. It raised circulating levels of high-density lipoprotein cholesterol. Sierra M.L., et al. 'Substituted 2-[(4-aminomethyl)phenoxy]-2-methylpropionic acid PPARalpha agonist. 1. Discovery of a novel series of potent HDLc raising agents.' J. Med. Chem. 50(4): 685-695 (2007). GW590735 potently increased high-density lipoprotein (HDL) cholesterol, decreased low-density lipoprotein (LDL) and very-low-density lipoprotein (VLDL) cholesterol, and significantly lowered triglycerides in human ApoB100/human CETP transgenic mice. Hansen M.K., et al. 'Selective CETP inhibition and PPARalpha agonism increase HDL cholesterol and reduce LDL cholesterol in human ApoB100/human CETP transgenic mice.' J. Cardiovasc. Pharmacol. Ther. 15(2): 196-202 (2010). Circulating FGF21 significantly increased in response to treatment with PPAR alpha (39%) and PPAR delta (32%), but not PPAR gamma agonist in humans. Christodoulides C., et al. 'Circulating fibroblast growth factor 21 is induced by peroxisome proliferator-activated receptor agonist but not ketosis in man.' J. Clin. Endocrinol. Metab. 94(9): 3594-3601 (2009).
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