Molecular Formula | C17H15N5O |
Molar Mass | 305.33 |
Density | 1.40±0.1 g/cm3(Predicted) |
Melting Point | >223°C (dec.) |
Solubility | DMSO: ≥ 33 mg/mL |
Appearance | powder |
Color | white to beige |
pKa | 12.96±0.50(Predicted) |
Storage Condition | room temp |
In vitro study | In macrophage Raw264.7, PF-06447475 inhibited its endogenous LRRK2 kinase activity with an IC50 of less than 10 nM. In astrocytes, PF-06447475 were able to rescue defects in lysosomal morphology and function due to LRRK2 mutations. |
In vivo study | In G2019S-LRRK2 transgenic mice (G2019S BAC-transgenic mice),PF-06447475 (100 mg/kg, p.o.) it can inhibit the phosphorylation of LRRK2 S935 and S1292 with IC50 of 103 nM and 21 nM, respectively. In G2019S-LRRK2 rats, PF-06447475 (30 mg/kg, p.o.) prevented α-synuclein-induced dopaminergic neurodegeneration and reduced neuroinflammation associated with G2019S-LRRK2 expression. |
Hazard Symbols | T - Toxic |
Risk Codes | 25 - Toxic if swallowed |
Safety Description | 45 - In case of accident or if you feel unwell, seek medical advice immediately (show the label whenever possible.) |
UN IDs | UN 2811 6.1 / PGIII |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 3.275 ml | 16.376 ml | 32.751 ml |
5 mM | 0.655 ml | 3.275 ml | 6.55 ml |
10 mM | 0.328 ml | 1.638 ml | 3.275 ml |
5 mM | 0.066 ml | 0.328 ml | 0.655 ml |
biological activity | PF-06447475 is an effective, selective LRRK2 kinase inhibitor that can penetrate into the brain, IC50 is 3 nM. |
target | TargetValue LRRK2 (Cell-free assay) 3nM G2019S LRRK2 (Cell-free assay) 11nM |
Target | Value |
LRRK2 (Cell-free assay) | 3nM |
G2019S LRRK2 (Cell-free assay) | 11nM |
in vitro study | in macrophage Raw264.7, PF-06447475 inhibited its endogenous LRRK2 kinase activity with IC50 less than 10 nM. In astrocytes, PF-06447475 can save lysosomal morphological and functional defects caused by LRRK2 mutation. |
in vivo study | in G2019S-LRRK2 transgenic mice (G2019S BAC-transgenic mice),PF-06447475 (100 mg/kg, p.o.) can inhibit phosphorylation of LRRK2 S935 and S1292 with IC50 of 103 nM and 21 nM respectively. In G2019S-LRRK2 rats, PF-06447475 (30 mg/kg, p.o.) can prevent α-synuclein-induced dopaminergic neurodegeneration and reduce neuroinflammation related to G2019S-LRRK2 expression. |