PLX5622 (hemifumarate)

453.45

DMSO : 100 mg/mL (ultrasonic); H₂O : 1 mg/mL (ultrasonic; warming; heat to 80C)

Protein Tyrosine Kinase/RTK

PLX5622 hemifumarate is a highly selective brain penetrant and orally active CSF1R inhibitor with an K_i of 5.9 nM, for extended and specific microglial elimination, preceding and during pathology development. PLX5622 hemifumarate demonstrates desirable PK properties in varies animals^[1][2]. IC50 & Target: CSF1R^[1] In Vivo: PLX5622 hemifumarate (1.2 g/kg; diet; for 14 days) can fully deplete CNS microglia^[3].
PLX5622 hemifumarate (65 mg/kg/day; oral gavage; for 14 days) causes paw withdrawal threshold high in males C57BL/6 mice (10-12 weeks old, 20-25 g), indicating that PLX5622 prevents the development of injury-associated mechanical allodynia^[2].