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PLX5622 {[allProObj[0].p_purity_real_show]}

货号:A1189464 Ambeed 开学季,买赠积分,赢豪礼

PLX5622 is a highly selective brain-penetrant CSF1R inhibitor allowing for extended and specific microglial elimination, preceding and during pathology development.

PLX5622 化学结构 CAS号:1303420-67-8
PLX5622 化学结构
CAS号:1303420-67-8
PLX5622 3D分子结构
CAS号:1303420-67-8
PLX5622 化学结构 CAS号:1303420-67-8
PLX5622 3D分子结构 CAS号:1303420-67-8
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PLX5622 纯度/质量文件 产品仅供科研

货号:A1189464 标准纯度: {[allProObj[0].p_purity_real_show]}
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PLX5622 生物活性

描述 icroglia are the resident immune cells in the central nervous system. The Colony-stimulating factor-1 receptor (CSF-1R) is expressed by microglia, macrophages and osteoclasts, and is required for their proliferation, differentiation, and survival. PLX5622 is an orally bioavailable, brain-penetrant and highly selective CSF-1R inhibitor with IC50 < 10 nM, showing > 20-fold selectivity over KIT and FLT3[1]. Oral PLX5622 (1200 ppM) treatment in 5xFAD mice model of Alzheimer’s disease with increased numbers of microglia/myeloid cells and masses of enlarged, plaque-associated cells throughout the brain led to almost complete microglial elimination (97–100% reduction), even with 24 weeks of treatment[1]. Approximately 99% of microglia were eliminated by embryonic day 15.5 (E15.5) and numbers of apoptotic cells accumulating throughout the developing hypothalamus were elevated after pregnant dams were placed on a PLX5622 diet starting at E3.5[2].
作用机制 PLX5622 is anchored to the active site of CSF1R by 3 hydrogen bonds. 7-Azaindole of PLX5622 forms two hydrogen bonds with the hinge region of CSF1R whereas the central pyridine ring forms a hydrogen bond with the main chain amino group of Phe796.

PLX5622 参考文献

[1]Spangenberg E, Severson PL, Hohsfield LA, Crapser J, Zhang J, Burton EA, Zhang Y, Spevak W, Lin J, Phan NY, Habets G, Rymar A, Tsang G, Walters J, Nespi M, Singh P, Broome S, Ibrahim P, Zhang C, Bollag G, West BL, Green KN. Sustained microglial depletion with CSF1R inhibitor impairs parenchymal plaque development in an Alzheimer's disease model. Nat Commun. 2019 Aug 21;10(1):3758. doi: 10.1038/s41467-019-11674-z. PMID: 31434879; PMCID: PMC6704256.

[2]Rosin JM, Vora SR, Kurrasch DM. Depletion of embryonic microglia using the CSF1R inhibitor PLX5622 has adverse sex-specific effects on mice, including accelerated weight gain, hyperactivity and anxiolytic-like behaviour. Brain Behav Immun. 2018 Oct;73:682-697. doi: 10.1016/j.bbi.2018.07.023. Epub 2018 Jul 27. PMID: 30056204.

PLX5622 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.53mL

0.51mL

0.25mL

12.65mL

2.53mL

1.26mL

25.29mL

5.06mL

2.53mL

PLX5622 技术信息

CAS号1303420-67-8
分子式C21H19F2N5O
分子量 395.405
别名
运输蓝冰
存储条件

粉末 Keep in dark place,Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 65 mg/mL(164.39 mM),配合低频超声,并水浴加热至45℃助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

无水乙醇: 3 mg/mL(7.59 mM),配合低频超声,并水浴加热至45℃助溶,注意:无水乙醇开封后,易挥发,也会吸收空气中的水分,导致溶解能力下降,请避免使用开封较久的乙醇

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