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Products are for research use only. Not for human use. We do not sell to patients.
(GW 1516; GSK-516; GW-501516)
GW 501516 Chemical Structure
|Product name: GW 501516|
|Cat. No.: HY-10838|
GW501516(GSK-516; GW1516) is a potent and highly selective PPARβ/δ agonist, with EC50 of 1 nM, with 1000-fold selectivity over hPPARα and hPPARγ.
IC50 Value: 1 nM(EC50)
in vitro: GW501516 is demonstrated to be 1000-fold more selective in comparison to existing subtypes. GW501516 increases expression of the reverse cholesterol transporter ATP-binding cassette A1 and induces apolipoprotein A1-specific cholesterol efflux In macrophages, fibroblasts, and intestinal cells. GW501516 can regulate expression of genes involved in lipid catabolism and energy uncoupling in skeletal muscle cells. Additionally, GW501516 is shown to block insulin resistance and fatty acid-induced nuclear factor-κB activation. GW 501516 reduces the IFNγ-induced up-regulation of TNFα and inducible NO synthase, and showed anti-inflammatory activity.
in vivo: GW501516 dramatically increases 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. GW501516 induces fatty acid β-oxidation in L6 myotubes and in mouse skeletal muscles. GW501516 treatment to mice fed a high-fat diet ameliorates diet-induced obesity as well as insulin resistance. GW501516 treatment also dramatically improves diabetes, as demonstrated by the decrease in plasma glucose and blood insulin levels in genetically obese ob/ob mice.
|M.Wt||453.5||Storage||Please store the product under the recommended conditions in the Certificate of Analysis.|
|Solvent & Solubility||
DMSO:50 mg/ml; DMF:25 mg/ml;methanol: 50 mg/ml;
|1 mg||5 mg||10 mg|
|1 mM||2.2051 mL||11.0254 mL||22.0507 mL|
|5 mM||0.4410 mL||2.2051 mL||4.4101 mL|
|10 mM||0.2205 mL||1.1025 mL||2.2051 mL|
. Barroso, Emma et al. The peroxisome proliferator-activated receptor .beta./.delta. (PPAR.beta./.delta.) agonist GW501516 prevents TNF-.alpha.-induced NF-.kappa.B activation in human HaCaT cells by reducing p65 acetylation through AMPK and SIRT1. Biochemical Pharmacology (2011) Volume: 81, Issue: 4, Pages: 534-543
. Ciocoiu CC, Ravna AW, Sylte I, Rustan AC, Hansen TV.Synthesis, molecular modeling studies and biological evaluation of fluorine substituted analogs of GW 501516.Bioorg Med Chem. 2011 Dec 1;19(23):6982-8. Epub 2011 Oct 17.
. Ciocoiu CC, Nikoli? N, Nguyen HH, Thoresen GH, Aasen AJ, Hansen TV.Synthesis and dual PPARalpha/delta agonist effects of 1,4-disubstituted 1,2,3-triazole analogues of GW 501516.Eur J Med Chem. 2010 Jul;45(7):3047-55. Epub 2010 Mar 27.
. Lu T, Chai Q, Yu L, d'Uscio LV, Katusic ZS, He T, Lee HC.Reactive oxygen species signaling facilitates FOXO-3a/FBXO-dependent vascular BK channel β1 subunit degradation in diabetic mice.Diabetes. 2012 Jul;61(7):1860-8. Epub 2012 May 14.
. Iwaisako K, Haimerl M, Paik YH, Taura K, Kodama Y, Sirlin C, Yu E, Yu RT, Downes M, Evans RM, Brenner DA, Schnabl B.Protection from liver fibrosis by a peroxisome proliferator-activated receptor δ agonist.Proc Natl Acad Sci U S A. 2012 May 22;109(21):E1369-76. Epub 2012 Apr 25.
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