• GW501516 is a potent and selective peroxisome proliferator-activated receptor (PPAR) β/δ modulator.
• In vitro, GW501516 increased expression of the reverse cholesterol transporter ATP-binding cassette A1 and induced apolipoprotein A1-specific cholesterol efflux. In vivo, GW501516 dramatically increased serum high density lipoprotein cholesterol while lowering the levels of small-dense low density lipoprotein, fasting triglycerides, and fasting insulin when dosed to insulin-resistant middle-aged obese rhesus monkeys. Oliver, W.R. Jr., et al. "A selective peroxisome proliferator-activated receptor δ agonist promotes reverse cholesterol transport." Proc. Natl. Acad. Sci. USA 98: 5306-5311 (2001).
• Treatment of skeletal muscle cells by GW501516 resulted in the expression of genes involved in lipid utilization, β-oxidation, cholesterol efflux, and energy uncoupling. Furthermore, the treatment also increased apolipoprotein-A1 specific efflux of intracellular cholesterol, indicating the muscle tissue is an important target of PPARβ/δ agonists. Dressel, U., et al. "The peroxisome proliferator-activated receptor β/δ agonist, GW501516, regulates the expression of genes involved in lipid catabolism and energy uncoupling in skeletal muscle cells." Mol. Endocrinol. 17: 2477-2493 (2003).
• GW501516 induced fatty acid β-oxidation in L6 myotubes and in mouse skeletal muscles. GW501516 treatment to mice fed a high-fat diet ameliorated diet-induced obesity as well as insulin resistance. GW501516 treatment also dramatically improved diabetes, as demonstrated by the decrease in plasma glucose and blood insulin levels in genetically obese ob/ob mice. Tanaka, T., et al. "Activation of peroxisome proliferator-activated receptor δ induces fatty acid β-oxidation in skeletal muscle and attenuates metabolic syndrome." Proc. Natl. Acad. Sci. USA 100: 15924-15929 (2003).
• GW501516 protected against cytotoxin-induced SH-SY5Y cell injury in vitro. It also significantly attenuated the ischemic brain damage and MPTP-induced depletion of striatal dopamine and related metabolite contents in mouse brain. Iwashita, A., et al. "Neuroprotective efficacy of the peroxisome proliferator-activated receptor δ-selective agonists in vitro and in vivo." J. Pharmacol. Exp. Ther. 320: 1087-1096 (2007).
• GW501516 treatment did not stimulate the growth of human cancer cell lines including HT29, HCT116, LS-174T, HepG2, and HuH7. Hollingshead, H.E., et al. "Peroxisome proliferator-activated receptor-β/δ (PPARβ/δ) ligands do not potentiate growth of human cancer cell lines." Carcinogenesis 28: 2641-2649 (2007).
• GW501516 was identified as an orally active agent that would mimic or potentiate the effects of exercise. Narkar, V.A., et al. "AMPK and PPARδ agonists are exercise mimetics." Cell 134: 405-415 (2008).
• GW 501516 reduced the IFNγ-induced up-regulation of TNFα and inducible NO synthase, and showed anti-inflammatory activity. Defaux, A., et al. "Effects of the PPAR-β agonist GW501516 in an in vitro model of brain inflammation and antibody-induced demyelination." J. Neuroinflammation 6: 15 (2009).
• Another CAS number previously assigned to GW501516 free acid, namely 813458-54-7, has been deleted by CAS and is no longer in use.
• STRUCTURE ERROR ON WIKIPEDIA'S GW501516 PAGE: As of December 21, 2012, the structure shown on the Wikipedia page for GW501516 is not correct -- the version shown on Wikipedia is missing a methyl group on the benzene ring carrying sulfur- and oxygen-bearing substituents.
• Sold for laboratory or manufacturing purposes only; not for human, veterinary, food, or household use.
• This product is offered for R&D use in accordance with (i) 35 USC 271(e)+A13(1) in the U.S.; (ii) Section 69.1 of Japanese Patent Law in Japan; (iii) Section 11, No. 2 of the German Patent Act of 1981 in Germany; (iv) Section 60, Paragraph 5b of the U.K. Patents Act of 1977 in the U.K.; (v) Sections 55.2(1) and 55.2(6) and other common law exemptions of Canadian patent law; (vi) Section 68B of the Patents Act of 1953 in New Zealand together with the amendment of same by the Statutes Amendment Bill of 2002; (vii) such related legislation and/or case law as may be or become applicable in the aforementioned countries; and (viii) such similar laws and rules as may apply in various other countries.
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