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MCS8874 PLX5622 [1303420-67-8]

MCS8874  PLX5622  [1303420-67-8]
MCS8874  PLX5622  [1303420-67-8] MCS8874  PLX5622  [1303420-67-8]

详情

描述 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。
靶点 CSF1R
分子式 C21H19F2N5O
CAS号 1303420-67-8
分子量 395.41
相关类别

信号通路 >> 蛋白酪氨酸激酶 >> c-FMS
研究领域 >> 神经疾病

动物实验

2-month-old wild-type mice were treated with vehicle or PLX5622 at 300- or 1200 mg/kg in chow for 7 or 21 days.2 month-old wild-type mice were treated with 300 or 1200 mg/kg PLX5622 or vehicle for 14 days, and LPS or PBS was then administered via IP (0.5 mg/kg).[1]

实验结果

[1] Microglial depletion does not affect behavior or learning and memory
The selective CSF1R inhibitor PLX5622 reduces microglial numbers in the adult brain



[2]Microglial elimination with PLX5622 followed by drug removal results in rapid repopulation of the CNS
Microglial elimination with PLX5622 followed by drug removal results in rapid repopulation of the CNS


[3]PLX5622 improves cognition in aged 3xTg-AD mice Lower-dose
PLX5622 improves cognition in aged 3xTg-AD mice


[4]PLX5622 treatment partially reduces microglial numbers
Lower-dose PLX5622 treatment partially reduces microglial numbers

溶解性 DMSO溶解度:79 mg/mL (199.79 mM)
Water溶解度:Insoluble
Ethanol溶解度:Insoluble
参考文献

[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]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.
[3]Huang Y, Xu Z, Xiong S, Sun F, Qin G, Hu G, Wang J, Zhao L, Liang YX, Wu T, Lu Z, Humayun MS, So KF, Pan Y, Li N, Yuan TF, Rao Y, Peng B. Repopulated microglia are solely derived from the proliferation of residual microglia after acute depletion. Nat Neurosci. 2018 Apr;21(4):530-540. doi: 10.1038/s41593-018-0090-8. Epub 2018 Feb 22. PMID: 29472620.
[4]Takeda A, Shinozaki Y, Kashiwagi K, Ohno N, Eto K, Wake H, Nabekura J, Koizumi S. Microglia mediate non-cell-autonomous cell death of retinal ganglion cells. Glia. 2018 Nov;66(11):2366-2384. doi: 10.1002/glia.23475. Epub 2018 Oct 29. PMID: 30375063.
[5]Liu Y, Given KS, Dickson EL, Owens GP, Macklin WB, Bennett JL. Concentration-dependent effects of CSF1R inhibitors on oligodendrocyte progenitor cells ex vivo and in vivo. Exp Neurol. 2019 Aug;318:32-41. doi: 10.1016/j.expneurol.2019.04.011. Epub 2019 Apr 25. PMID: 31029597; PMCID: PMC6615458.

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