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. The PPARβ/δ agonist GW501516 inhibited the increase caused by TNF-α in the mRNA levels of the NF-κB target genes interleukin 8 (IL-8), TNF-α and thymic stromal lymphopoietin (TSLP). GW501516 exhibited agonist effects with EC(50) values of 560 and 55 nM against PPARα and PPARδ, respectively, in a luciferase assay. Moreover, GW501516 also exhibited potent ability to induce oleic acid oxidation in a human myotube cell assay with EC(50)=3.7 nM. In contrast, GW501516 treatment decreased TNF-α-induced p65 acetylation. GW501516 increased AMPK phosphorylation and the subsequent p300 phosphorylation, leading to a marked reduction in the association between p65 and this transcriptional co-activator.
|Source||Oncotarget (2017). Figure 1. GW501516|
|Cell Lines||MDA-MB-231, MDA-MB-435, and ZR-75-1 cells|
|Incubation Time||48 h|
|Results||Consistent with the results in MDA-MB-231 cells, the migration of other high metastatic human breast cancer cell lines MDA-MB-435 and ZR-75-1 was dose-dependently inhibited in the presence of GW501516|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
Reactive oxygen species signaling facilitates FOXO-3a/FBXO-dependent vascular BK channel β1 subunit degradation in diabetic mice.
Lu T, et al. Diabetes. 2012 Jul;61(7):1860-8. PMID: 22586590.
Protection from liver fibrosis by a peroxisome proliferator-activated receptor δ agonist.
Iwaisako K, et al. Proc Natl Acad Sci U S A. 2012 May 22;109(21):E1369-76. PMID: 22538808.
Synthesis, molecular modeling studies and biological evaluation of fluorine substituted analogs of GW 501516.
Ciocoiu CC, et al. Bioorg Med Chem. 2011 Dec 1;19(23):6982-8. PMID: 22051054.
The peroxisome proliferator-activated receptor β/δ (PPARβ/δ) agonist GW501516 prevents TNF-α-induced NF-κB activation in human HaCaT cells by reducing p65 acetylation through AMPK and SIRT1.
Barroso E, et al. Biochem Pharmacol. 2011 Feb 15;81(4):534-43. PMID: 21146504.
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