PF-06447475 - 99%, high purity , CAS No.1527473-33-1, Inhibitor of leucine rich repeat kinase 2

Item Number

P413944

• Synonyms: PF-06447475|1527473-33-1|PF06447475|3-(4-morpholino-7H-pyrrolo[2,3-d]pyrimidin-5-yl)benzonitrile|3-[4-(morpholin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile|CHEMBL3393348|PF 06447475|3-(4-(morpholin-4-yl)-7h-pyrrolo[2,3-d]pyrimidin-5-yl)benzonitril
• Specifications & Purity: Moligand™, ≥99%
• Biochemical and Physiological Mechanisms: PF-06447475 is a potent, selective, and brain penetrant LRRK2 kinase inhibitor with IC50 of 3 nM.
• Storage Temp: Store at -20°C
• Shipped In: Ice chest + Ice pads
• Grade: Moligand™
• Action Type: INHIBITOR
• Mechanism of action: Inhibitor of leucine rich repeat kinase 2

Product Description

Information

PF-06447475 PF-06447475 is a potent, selective, and brain penetrant LRRK2 kinase inhibitor with IC50 of 3 nM.

Targets

LRRK2 (Cell-free assay); G2019S LRRK2 (Cell-free assay) 3nM; 11nM

In vitro

In the macrophage cell line Raw264.7, PF-06447475 inhibits endogenous LRRK2 kinase activity with IC50 of <10 nM. In astrocytes, PF-06447475 rescues LRRK2 mutation-induced defects in lysosomal morphology and function.

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. 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.