2019年8月21日 · Microglia are dependent on colony-stimulating factor 1 receptor (CSF1R) signaling for their survival. We designed and synthesized a highly selective brain-penetrant CSF1R inhibitor...

PLX5622 is a highly selective brain penetrant and orally active CSF1R inhibitor (IC 50 =0.016 μM; K i =5.9 nM). PLX5622 allows for extended and specific microglial cells elimination, preceding and during pathology development. PLX5622 demonstrates desirable PK properties in varies animals.

2023年12月1日 · High-dose application of the colony stimulating factor 1 receptor (CSF1R) inhibitor PLX5622 (1200 ppm) seven days prior to sepsis induction lead to 70–80% microglia reduction but resulted in fatal outcome of bacterial sepsis or LPS induced inflammation.

PLX5622是一种针对CSF1R（巨噬细胞集落刺激因子1受体）的抑制剂，它用于小胶质细胞（microglia）的清除。 小胶质细胞是中枢神经系统中的主要免疫细胞类型，负责监测和调节神经组织中的炎症反应和损伤修复。

PLX5622 is a potent inhibitor of CSF1R tyrosine kinase activity (KI = 5.9 nM) with at least 50-fold selectivity over 4 related kinases, and over 100-fold selectivity against a panel of 230 kinases [11 – 14].

2025年3月14日 · PLX5622, a selective CSF1R inhibitor, has become a widely used tool for studying microglial dynamics by enabling controlled depletion and repopulation. Understanding its mechanism and effects is essential for evaluating its potential in neuroscience research and therapeutic development.

2019年8月21日 · Microglia are dependent on colony-stimulating factor 1 receptor (CSF1R) signaling for their survival. We designed and synthesized a highly selective brain-penetrant CSF1R inhibitor (PLX5622) allowing for extended and specific microglial elimination, preceding and during pathology development.

2022年4月2日 · PLX3397 (Pexidartinib) and PLX5622 are the most widely used CSF-1R inhibitors, with favorable tolerability profiles. Treatment with PLX3397, or PLX5622, causes effective depletion of microglia. PLX3397 also inhibits C-KIT, PDGFRα and FLT3.

2022年3月25日 · PLX5622 is a CSF-1R inhibitor and microglia-depleting reagent, widely used to investigate the biology of this central nervous system (CNS)-resident myeloid population, but the indirect or off-target effects of this agent remain largely unexplored.

PLX5622 is a highly selective brain penetrant and oral active CSF1R inhibitor. PLX5622 has been shown to eliminate microglia from the brain, which can be sustained in wild-type and the Alzheimer's disease model mice (3xTg-AD model).