| Name | PF-06447475 |
| Description | PF-06447475 is a highly effective, specific, brain penetrant LRRK2 inhibitor with IC0 of 3/11 nM for wild type LRRK2 and G2019S LRRK2 respectively. |
| In vitro | In the macrophage cell line Raw264.7, PF-06447475 inhibits endogenous LRRK2 kinase activity with IC50 of <10 nM. [2] In astrocytes, PF-06447475 rescues LRRK2 mutation-induced defects in lysosomal morphology and function. [3] |
| In vivo | In G2019S BAC-transgenic mice, PF-06447475 (100 mg/kg, p.o.) inhibits pS935 and pS1292 phosphorylation of LRRK2 with IC50 of 103 nM and 21 nM, respectively. [1] In G2019S-LRRK2 rats, PF-06447475 (30 mg/kg, p.o.) blocks α-synuclein-induced dopaminergic neurodegeneration and attenuates neuroinflammation associated with G2019S-LRRK2 expression. [2] |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 15.3 mg/mL (50 mM)
|
| Keywords | Inhibitor | Leucine-rich repeat kinase 2 | LRRK2 | inhibit | PF06447475 | PF 06447475 | PF-06447475 |
| Inhibitors Related | PFE-360 | GNE0877 | CZC-25146 | GSK2578215A | GNE-9605 | CZC-54252 hydrochloride | GNE-7915 | EB-42486 | LRRK2 inhibitor 1 | LRRK2-IN-7 | LRRK2-IN-1 | CCG-1423 |
| Related Compound Libraries | Bioactive Compound Library | Anti-Neurodegenerative Disease Compound Library | Kinase Inhibitor Library | Autophagy Compound Library | Anti-Parkinson's Disease Compound Library | CNS-Penetrant Compound Library | Inhibitor Library | NO PAINS Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max |
United States
