Molecular Formula | C21H18F3NO3S2 |
Molar Mass | 453.5 |
Density | 1.42±0.1 g/cm3(Predicted) |
Melting Point | 134-136°C |
Boling Point | 584.5±60.0 °C(Predicted) |
Flash Point | 307.321°C |
Solubility | DMSO: soluble20mg/mL, clear |
Vapor Presure | 0mmHg at 25°C |
Appearance | powder |
Color | white to beige |
BRN | 18515150 |
pKa | 3.17±0.10(Predicted) |
Storage Condition | -20°C |
Stability | Light Sensitive |
Refractive Index | 1.619 |
In vitro study | GW 501516 is shown to be the most potent and selective PPARα agonists known with an EC 50 of 1.1 nM against PPARα and 1000-fold selectivity over the other human subtypes, PPARα and-γ. GW 501516 exerts anti-inflammatory effects in mouse cultured proximal tubular (mProx) cells. GW 501516 inhibits palmitate- and TNFα-induced increases in MCP-1 mRNA expression in a dose-dependent manner. |
In vivo study | GW 501516 causes impaired bone formation, leading to decreased BMD and deterioration of bone properties in OVX rats. GW 501516 attenuates interstitial inflammation and proximal tubular cell damage in a protein-overload mouse nephropathy model. GW 501516 treatment enhances running endurance and the proportion of succinate dehydrogenase (SDH)-positive muscle fibres in both trained and untrained mice. |
WGK Germany | 3 |
RTECS | AI9105500 |
biological activity | GW 501516 (GW 1516) is an agonist of PPARδ with an EC50 value of 1.1 nM. |
Target | Value |
PPARδ (Cell-free assay) | 1 nM(Ki) |