GW501516 is a selective PPARd agonist with a Ki affinity of 1.1 nM in a human binding assay. In a cell-based transfection assay, GW501516 induces expression of GAL4-responsive reporter gene at an EC50 of 1.2 nM. At doses up to 1 uM, GW501516 does not promote adipocyte differentiation, bind to RXRa, or have activity toward other nuclear or non-nuclear receptors. (1) GW501516 incrases expression of the reverse cholesterol transporter ATP-binding cassette A1 and induces apolipoprotein A1-specific cholesterol efflux. (1)
GW501516 is also reported to be a PPARb agonist with anti-inflammatory activity and decreases IFN-g-induced upregulation of TNF-a and iNOS. Concurrently, GW501516 increase IL-6 mRNA expression. (2)
Technical information:
| Chemical Formula: | C21H18F3NO3S2 | |
| CAS #: | 317318-70-0 | |
| Molecular Weight: | 453.5 | |
| Purity: | > 98% | |
| Appearance: | white | |
| Chemical Name: | 2-(2-methyl-4-((4-methyl-2-(4-(trifluoromethyl)phenyl)thiazol-5-yl)methylthio)phenoxy)acetic acid | |
| Solubility: | Up to 22 mM in DMSO | |
| Synonyms: | GW501516, GW-501,516, GW1516, GSK-516, Endurobol |
Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.
Reference:
| 1. | Oliver et al., A selective peroxisome proliferator-activated receptor d agonist promotes reverse cholesterol transport. Proc. Nat'l. Acad. Sci. 2001, 98(9), 5306-5311. Pubmed ID: 11309497 |
| 2. | Defaux et al., Effects of the PPAR-b agonist GW501516 in an in vitro model of brain inflammation and antibody-induced demyelination. J. Neuroinflammation, 2009, 6, 15-27. Pubmed ID: 19422681 |
Other Information:
Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.
