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GW501516

AG-CR1-3641-M001 1 mg $25.00
AG-CR1-3641-M005 5 mg $65.00
AG-CR1-3641-M025 25 mg $260.00
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Additional Information

Product Data
Synonyms GSK-516; GW1516; Endurobol; 2-[2-Methyl-4-[[[4-methyl-2-[4-(trifluoromethyl)phenyl]-5-thiazolyl]methyl]thio]phenoxy]acetic acid
Properties
Formula C21H18F3NO3S2
MW 453.5
CAS 317318-70-0
RTECS AI9105500
Purity ≥98% (NMR)
Appearance White to off-white solid.
Solubility Soluble in DMSO (30mg/ml), dimethylformamide (30mg/ml), ethanol (10mg/ml) or methanol (30mg/ml). Sparingly soluble in water.
Identity Identity determined by 1H-NMR / 13C-NMR.
InChi Key YDBLKRPLXZNVNB-UHFFFAOYSA-N
Product Type Chemical
Shipping and Handling
Shipping AMBIENT
Short Term Storage +4°C
Long Term Storage -20°C
Handling Advice Keep cool and dry.
Use/Stability Stable for at least 2 years after receipt when stored at -20°C.
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Product Description

  • Potent and selective peroxisome proliferator-activated receptor (PPAR) δ agonist/activator with high affinity (Ki=1nM) and potency (EC50=1nM) for PPARδ and >1000 fold selectivity over PPARα and PPARγ. The peroxisome proliferator-activated receptor δ (PPAR δ) has emerged as an important regulator of lipid homeostasis and inflammatory signaling. Recent in vitro, in vivo and human clinical studies have highlighted a role for PPARδ activation in the prevention and treatment of insulin resistance and atherosclerosis.
  • Antidiabetic compound.
  • Shown to activate pathways initiated through exercise and was investigated as a potential treatment for obesity, diabetes, dyslipidemia and cardiovascular disease. Off-target high doses lead to tumor progression in rodents.
  • Increases ABC A1 transporter expression and induces apolipoprotein A1-mediated cholesterol efflux in vitro.
  • Increase serum HDL cholesterol and lowers small-dense LDL levels in obesity in vivo models.
  • Reduces plasma triglyceride concentration.
  • Increases expression of genes involved in lipid utilization, β-oxidation, cholesterol efflux and energy uncoupling, as well as apolipoprotein-A1 specific efflux of intracellular cholesterol, indicating the muscle tissue is an important target.
  • Model compound for a new type of obesity therapeutic, as well as a selective pharmacological tool for understanding lipid metabolism.

Product References

  1. A selective peroxisome proliferator-activated receptor delta agonist promotes reverse cholesterol transport: W.R. Oliver, et al.; PNAS 98, 5306 (2001)
  2. Novel selective small molecule agonists for peroxisome proliferator-activated receptor delta (PPARdelta)-synthesis and biological activity: M.L. Sznaidman, et al.; Bioorg. Med. Chem. Lett. 13, 1517 (2003)
  3. The peroxisome proliferator-activated receptor beta/delta agonist, GW501516, regulates the expression of genes involved in lipid catabolism and energy uncoupling in skeletal muscle cells: U. Dressel, et al.; Mol. Endocrinol. 17, 2477 (2003)
  4. Activation of peroxisome proliferator-activated receptor delta induces fatty acid beta-oxidation in skeletal muscle and attenuates metabolic syndrome: T. Tanaka, et al.; PNAS 100, 15924 (2003)
  5. Peroxisome proliferator-activated receptor delta and gamma agonists differentially alter tumor differentiation and progression during mammary carcinogenesis: Y. Yin, et al.; Cancer Res. 65, 3950 (2005)
  6. Activation of PPARbeta/delta induces endothelial cell proliferation and angiogenesis: L. Piqueras, et al.; Arterioscler. Thromb. Vasc. Biol. 27, 63 (2007)
  7. AMPK and PPARdelta agonists are exercise mimetics: V.A. Narkar, et al.; Cell 134, 405 (2008)
  8. Peroxisome proliferator-activated receptor delta agonists inhibit T helper type 1 (Th1) and Th17 responses in experimental allergic encephalomyelitis: S. Kanakasabai, et al.; Immunol. 130, 572 (2010)
  9. Activation of PPARδ promotes mitochondrial energy metabolism and decreases basal insulin secretion in palmitate-treated β-cells: L. Jiang, et al.; Mol. Cell Biochem. 343, 249 (2010)
  10. Activation of peroxisome proliferator-activated receptor-{delta} by GW501516 prevents fatty acid-induced nuclear factor-{kappa}B activation and insulin resistance in skeletal muscle cells: T. Coll, et al.; Endocrinol. 151, 1560 (2010)
  11. The role played by the peroxisome proliferator-activated receptor-β/δ (PPARβ/δ) activator, GW501516, in control of fatty acid metabolism: a new potential therapeutic target for treating metabolic syndrome: J. Lee & W.Y. Chung; Endocrinol. 152, 1742 (2011)
  12. Peroxisome proliferator-activated receptor δ: a multifaceted metabolic player: L.A. Bojic & M.W. Huff; Curr. Opin. Lipidol. 24, 171 (2013) (Review)
  13. Harnessing the benefits of PPARβ/δ agonists: L.S. Mackenzie & L. Lione; Life Sci. 93, 963 (2013) (Review)
  14. Short-term administration of GW501516 improves inflammatory state in white adipose tissue and liver damage in high-fructose-fed mice through modulation of the renin-angiotensin system: D.C. Magliano, et al.; Endocrine 50, 355 (2015)
  15. Unraveling the Effects of PPARβ/δ on Insulin Resistance and Cardiovascular Disease: M. Vazquez-Carrera; Trends Endocrinol. Metab. 27, 319 (2016) (Review)
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