GW501516
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.
Catalog Number | AG-CR1-3641-M001 |
Alternative Name(s) | GSK-516; GW1516; Endurobol; 2-[2-Methyl-4-[[[4-methyl-2-[4-(trifluoromethyl)phenyl]-5-thiazolyl]methyl]thio]phenoxy]acetic acid |
Research Area | Biochemicals, Immunology, Metabolism |
Molecular Formula | C21H18F3NO3S2 |
CAS# | 317318-70-0 |
Purity | >98% |
Inchi | InChI=1S/C21H18F3NO3S2/c1-12-9-16(7-8-17(12)28-10-19(26)27)29-11-18-13(2)25-20(30-18)14-3-5-15(6-4-14)21(22,23)24/h3-9H,10-11H2,1-2H3,(H,26,27) |
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 |
Size | 1 mg |
Supplier Page | http://www.adipogen.com/ag-cr1-3641/gw501516.html |