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ProductsBack/GW501516 [317318-70-0]
Chemical Structure
Chemical Structure
Chemical Structure

GW501516 [317318-70-0]

Research Use Only
AG-CR1-3641
AdipoGen Life Sciences
CAS Number317318-70-0
DownloadMSDS
Product group Chemicals
Estimated Purity>98%
Molecular Weight453.5
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Overview

  • Supplier
    AdipoGen Life Sciences
  • Product Name
    GW501516 [317318-70-0]
  • Delivery Days Customer
    10
  • CAS Number
    317318-70-0
  • Certification
    Research Use Only
  • Estimated Purity
    >98%
  • Molecular Formula
    C21H18F3NO3S2
  • Molecular Weight
    453.5
  • Scientific Description
    Chemical. CAS: 317318-70-0. Formula: C21H18F3NO3S2. MW: 453.5. Potent and selective peroxisome proliferator-activated receptor (PPAR) delta agonist/activator with high affinity (Ki=1nM) and potency (EC50=1nM) for PPARdelta and >1000 fold selectivity over PPARalpha and PPARgamma. The peroxisome proliferator-activated receptor delta (PPAR delta) 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 PPARdelta 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, beta-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. - Potent and selective peroxisome proliferator-activated receptor (PPAR) delta agonist/activator with high affinity (Ki=1nM) and potency (EC50=1nM) for PPARdelta and >1000 fold selectivity over PPARalpha and PPARgamma. The peroxisome proliferator-activated receptor delta (PPAR delta) 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 PPARdelta 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, beta-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.
  • SMILES
    CC1=CC(SCC2=C(C)N=C(C3=CC=C(C(F)(F)F)C=C3)S2)=CC=C1OCC(O)=O
  • Storage Instruction
    -20°C,2°C to 8°C
  • UNSPSC
    12352200

References

  • A selective peroxisome proliferator-activated receptor delta agonist promotes reverse cholesterol transport: W.R. Oliver, et al.; PNAS 98, 5306 (2001)
  • 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)
  • 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)
  • 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)
  • 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)
  • Activation of PPARbeta/delta induces endothelial cell proliferation and angiogenesis: L. Piqueras, et al.; Arterioscler. Thromb. Vasc. Biol. 27, 63 (2007)
  • AMPK and PPARdelta agonists are exercise mimetics: V.A. Narkar, et al.; Cell 134, 405 (2008)
  • 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)
  • Activation of PPARdelta promotes mitochondrial energy metabolism and decreases basal insulin secretion in palmitate-treated beta-cells: L. Jiang, et al.; Mol. Cell Biochem. 343, 249 (2010)
  • 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)