Molecular Formula | C17H20ClF4N7O |
Molar Mass | 449.83 |
Density | 1.67±0.1 g/cm3(Predicted) |
Boling Point | 587.9±60.0 °C(Predicted) |
Solubility | DMSO: ≥ 60 mg/mL |
pKa | 5.04±0.60(Predicted) |
Storage Condition | Keep in dark place,Inert atmosphere,Store in freezer, under -20°C |
In vitro study | GNE-9605 was highly effective against LRRK2 in both biochemical (Ki = 2.0 nM) and cellular (IC50=19 nM) assays. Of the in vitro human MDR1 permeability data, GNE-9605 showed good brain permeability in higher species. |
In vivo study | In vivo rat PK studies showed that GNE-9605 (1 mg/kg, p.o.) with a total plasma clearance of 26 mL/min/kg and good oral bioactivity (90%). In G2019S Parkinson's disease mutant BAC transgenic mice expressing human LRRK2 protein, GNE-9605 (10 and 50 mg/kg, I. p.) inhibited LRRK2 Ser1292 autophosphorylation in vivo. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.223 ml | 11.115 ml | 22.23 ml |
5 mM | 0.445 ml | 2.223 ml | 4.446 ml |
10 mM | 0.222 ml | 1.112 ml | 2.223 ml |
5 mM | 0.044 ml | 0.222 ml | 0.445 ml |