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AdipoGen Life Sciences
GW501516
35
CHF
CHF 35.00
In stock
AG-CR1-3641-M0011 mgCHF 35.00
AG-CR1-3641-M0055 mgCHF 90.00
AG-CR1-3641-M02525 mgCHF 350.00
| Product Details | |
|---|---|
| Synonyms | GSK-516; GW1516; Endurobol; 2-[2-Methyl-4-[[[4-methyl-2-[4-(trifluoromethyl)phenyl]-5-thiazolyl]methyl]thio]phenoxy]acetic acid |
| Product Type | Chemical |
| Properties | |
| Formula |
C21H18F3NO3S2 |
| MW | 453.5 |
| CAS | 317318-70-0 |
| RTECS | AI9105500 |
| Purity Chemicals | ≥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 |
| Smiles | CC1=CC(SCC2=C(C)N=C(C3=CC=C(C(F)(F)F)C=C3)S2)=CC=C1OCC(O)=O |
| 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. |
| Documents | |
| MSDS |
 Download PDF |
| Product Specification Sheet | |
| Datasheet |
Download PDF |
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
- 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 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)
- 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)
- 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)
- Peroxisome proliferator-activated receptor δ: a multifaceted metabolic player: L.A. Bojic & M.W. Huff; Curr. Opin. Lipidol. 24, 171 (2013) (Review)
- Harnessing the benefits of PPARβ/δ agonists: L.S. Mackenzie & L. Lione; Life Sci. 93, 963 (2013) (Review)
- 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)
- Unraveling the Effects of PPARβ/δ on Insulin Resistance and Cardiovascular Disease: M. Vazquez-Carrera; Trends Endocrinol. Metab. 27, 319 (2016) (Review)
- Remodeling of metabolism and inflammation by exercise ameliorates tumor-associated anemia: R. Furrer, et al.; Sci. Adv. Immunol. 7, 37 (2021)
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