PLX5622 是高度选择性的、能透过血脑屏障的、口服有效的 CSF1R 抑制剂，可用于病程发展前和过程中，扩大的和特异性的小胶质细胞的消除。 PLX5622 具有较好的药理学特性。 Information PLX5622 PLX5622 is a highly selective CSF-1R inhibitor (IC50 20-fold selectivity over KIT and FLT3. Targets CSF-1R (Cell-free assay); FLT3 (Cell-free assay); KIT (Cell-free assay); AURKC (Cell-free assay); KDR (Cell-free assay) ;0.016 μM; 0.39 μM; 0.86 μM; 1 μM; 1.1 μM In vivo In vivo PLX5622 demonstrates desirable PK properties in mice, rats, dogs, and monkeys, with a brain penetrance of ~20%. PLX5622 has low systemic clearance, moderate volume of distribution, and favorable oral bioavailability (F > 30%) in all four species. PLX5622 is a useful compound for investigating microglial dynamics. It allows for the sustained and specific elimination of microglia, preceding and during pathology development of Alzheimer’s disease (AD). Long-term PLX5622-mediated microglial depletion is highly robust, sustainable, and specific to the microglial compartment.