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Cat. No. M3658
GW501516 Structure

GSK-516, GW1516

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
5mg USD 49 In stock
10mg USD 77 In stock
50mg USD 185 In stock
100mg USD 260 In stock
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Quality Control
Biological Activity

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.

Customer Product Validations & Biological Datas
Source Oncotarget (2017). Figure 1. GW501516
Method migration assay
Cell Lines MDA-MB-231, MDA-MB-435, and ZR-75-1 cells
Concentrations 100 nM
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
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
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.

Chemical Information
Molecular Weight 453.5
Formula C21H18F3NO3S2
CAS Number 317318-70-0
Purity 99.83%
Solubility DMSO 47 mg/mL
Storage at -20°C

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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Abmole Inhibitor Catalog 2017

Keywords: GW501516, GSK-516, GW1516 supplier, PPAR, inhibitors

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