Molecular Formula | C14H16F3N7 |
Molar Mass | 339.32 |
Density | 1.36±0.1 g/cm3(Predicted) |
Melting Point | 121 - 122°C |
Boling Point | 506.3±60.0 °C(Predicted) |
Solubility | DMSO (Slightly), Methanol (Slightly) |
Appearance | Solid |
Color | White to Off-White |
pKa | 3.87±0.10(Predicted) |
Storage Condition | -20°C, Inert atmosphere |
In vitro study | GNE-0877 significantly inhibited LRRK2 cell activity with an IC50 of 3 nM and showed low conversion in human liver microsomes and hepatocytes. In addition, GNE-0877 was also a reversible CYP1A2 inhibitor with an IC50 of 0.7 μm. GNE-0877 significantly inhibited LRRK2 cell activity with an IC50 of 3 nM and showed low conversion in human liver microsomes and hepatocytes. In addition, GNE-0877 was also a reversible CYP1A2 inhibitor with an IC50 of 0.7 μm. |
In vivo study | In vivo, GNE-0877 showed good oral bioavailability and brain permeability. In BAC transgenic mice containing a G2019S Parkinson's disease mutant that expresses human LRRK2 protein, GNE-0877 inhibited LRRK2 Ser1292 autophosphorylation in vivo. In vivo, GNE-0877 showed good oral bioavailability and brain permeability. In BAC transgenic mice containing a G2019S Parkinson's disease mutant that expresses human LRRK2 protein, GNE-0877 inhibited LRRK2 Ser1292 autophosphorylation in vivo. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.947 ml | 14.735 ml | 29.471 ml |
5 mM | 0.589 ml | 2.947 ml | 5.894 ml |
10 mM | 0.295 ml | 1.474 ml | 2.947 ml |
5 mM | 0.059 ml | 0.295 ml | 0.589 ml |