PF-06447475是一种高效、特异性的脑渗透性 LRRK2 抑制剂，IC50值为3 nM。

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 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 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]

1527473-33-1

C17H15N5O

305.33

DMSO:15.3 mg/mL (50 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years