Molecular Formula | C17H12F9NO3S |
Molar Mass | 481.33 |
Density | 1.550±0.06 g/cm3(Predicted) |
Melting Point | 116-118°C |
Boling Point | 470.5±55.0 °C(Predicted) |
Solubility | DMSO (Slightly), Methanol (Slightly) |
Appearance | Light beige solid |
Color | Off-White |
pKa | 9.00±0.15(Predicted) |
Storage Condition | -20°C |
In vitro study | T-0901317 acts through LXR, consistent with its RXR heterodimer partner inducing ABCA1 to reverse the expression of cholesterol transporter. T-0901317 upregulates ABCA1 gene expression associated with regulation of cholesterol efflux and HDL metabolism. T-0901317 activates the bile acid farnesoid X receptor (FXR) with an EC50 of 5 μm, which is 10 times more effective than the natural FXR ligand chenodeoxy acid acid. T-0901317 is also a high affinity ligand for the exogenous receptor pregnane X receptor (PXR). T-0901317 binds and activates PXR with the same nanomolar potency as it stimulates LXR activity. T-0901317 acts on cells and animals to induce not only LXR target gene expression, but also PXR target gene expression, including scavenger receptor CD36. T-0901317 acts on primary neurons in vitro to reduce β-amyloid production. T0901317 binds directly with high affinity to RORα and RORγ (K I = 132 and 51 nM, respectively) and modulates receptor interaction with transcription cofactor proteins. T09901317 inhibits ROR α/γ-dependent transactivation of ROR response reporter gene, reducing steroid receptor coactivator -2 in HepG2 cells in the endogenous ROR target gene (G6Pase) on recruitment. |
In vivo study | Treatment of 11-week-old APP23 mice with t-0901317 for 6 days significantly increased ABCA1 expression and decreased the ratio of soluble APP(sAPP)β to sapα cleavage products. Most importantly, this treatment statistically significantly reduced soluble Aβ40 and Aβ42 levels in the mouse brain. |
WGK Germany | 3 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.078 ml | 10.388 ml | 20.776 ml |
5 mM | 0.416 ml | 2.078 ml | 4.155 ml |
10 mM | 0.208 ml | 1.039 ml | 2.078 ml |
5 mM | 0.042 ml | 0.208 ml | 0.416 ml |