PLX5622 hemifumarate 是高度选择性的、能透过血脑屏障的、口服有效的 CSF1R 抑制剂，Ki 值为 5.9 nM，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 hemifumarate 具有较好的药理学特性。
货号:ajcx15456
CAS:N/A
分子式:C23H21F2N5O3
分子量：453.45
溶解度:DMSO: 100 mg/mL (220.53 mM); H2O:< 0.1 mg/mL (insoluble)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

PLX5622 hemifumarate is a highly selective brain penetrant and oral active CSF1R inhibitor with an Ki 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].

PLX5622 hemifumarate (oral gavage; 65 mg/kg/day; for 14 days) causes paw withdrawal threshold high in mice, indicating that PLX5622 prevents the development of injury-associated mechanical allodynia[2]. Animal Model: C57BL/6 mice (males, 10-12 weeks old, 20-25 g)[2]

[1]. Spangenberg E, et al. Sustained microglial depletion with CSF1R inhibitor impairs parenchymal plaque development in an Alzheimer's disease model. Nat Commun. 2019 Aug 21;10(1):3758. [2]. Lee S, et al. Targeting macrophage and microglia activation with colony stimulating factor 1 receptor inhibitor is an effective strategy to treat injury-triggered neuropathic pain. Mol Pain. 2018 Jan-Dec;14:1744806918764979.