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Description
PLX-5622 is a highly selective brain-penetrant CSF1R inhibitor (IC50=0.016 µM; Ki=5.9 nM) allowing for extended and specific microglial elimination, preceding and during pathology development.
Key Features
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CSF1R Inhibition: PLX-5622 selectively targets and inhibits CSF1R, which is essential for the survival and function of microglia. This leads to a reversible depletion of microglia in animal models.
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Brain-Penetrant: The compound efficiently crosses the blood-brain barrier, making it effective for CNS-related research.
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Microglia Depletion: It has been shown to achieve over 90% depletion of microglia in rodent models within a short time frame.
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Reversibility: Microglial depletion by PLX-5622 is reversible, allowing researchers to study the reconstitution of these cells and their role in health and disease.
PLX-5622 has become invaluable for studying not only neurodegenerative diseases but also neuroinflammation and immune responses in the brain. By removing microglia, researchers can better understand their intricate roles and potential as therapeutic targets, offering insights into both the inflammatory processes and the overall immune regulation in the central nervous system. This reversible microglia depletion makes PLX-5622 an essential tool for investigating the dynamic interactions between microglia, inflammation, and neurodegeneration.
Comments
100% purity. The bioactivity of PLX-5622 has been demonstrated satisfactorily in diet depletion studies in rodents.
95-100% microglia depletion after only 5 days of dietary administration from Harvard Medical School.
Specification
| Product Name | PLX-5622 |
| Chemical Formula | C21H19F2N5O |
| Molecular Weight | 395.41 |
| CAS# | 1303420-67-8 |
| Appearance | Solid powder |
| Purity | > 99% by HPLC |
| Solubility | Soluble in DMSO |
| Storage | Room temperature for months, or -20℃ for 3 years |
| Targets | CSF-1R |
| Synonym | PLX-5622; PLX5622; PLX 5622 |
| SMILES Code | CC1=CN=C2C(C(CC3=C(F)N=C(NCC4=CC(F)=CN=C4OC)C=C3)=CN2)=C1 |
References
Science. 2024 Jun 21;384(6702):eadh5548. doi: 10.1126/science.adh5548. Epub 2024 Jun 21.
Breast cancer exploits neural signaling pathways for bone-to-meninges metastasis.
Andrew E Whiteley # 1, Danhui Ma # 1, Lihua Wang 1, Seok-Yeong Yu 1, Claire Yin 1, Trevor T Price 1, Brennan G Simon 1, Katie R Xu 1, Kathleen A Marsh 1, Maegan L Brockman 1, Tatiana M Prioleau 1, Katherine I Zhou 1, Xiuyu Cui 2, Peter E Fecci 2, William R Jeck 3, Chad M McCall 3, Jadee L Neff 3, Dorothy A Sipkins 1
Nature Neuroscience. 2023 Oct 17:2023.10.17.562708. doi: 10.1101/2023.10.17.562708.
Microglia are dispensable for experience-dependent refinement of mouse visual circuitry.
Thomas C Brown 1, Emily C Crouse 1, Cecilia A Attaway 1, Dana K Oakes 1, Sarah W Minton 1, Bart G Borghuis 1, Aaron W McGee 1
Nature. 2023 Jan;613(7942):120-129. doi: 10.1038/s41586-022-05534-y.
Microglia regulate central nervous system myelin growth and integrity.
McNamara NB, Munro DAD, Bestard-Cuche N, Uyeda A, Bogie JFJ, Hoffmann A, Holloway RK, Molina-Gonzalez I, Askew KE, Mitchell S, Mungall W, Dodds M, Dittmayer C, Moss J, Rose J, Szymkowiak S, Amann L, McColl BW, Prinz M, Spires-Jones TL, Stenzel W, Horsburgh K, Hendriks JJA, Pridans C, Muramatsu R, Williams A, Priller J, Miron VE.
Cell Rep. 2022 Aug 16;40(7):111209.
Microglia contribute to the postnatal development of cortical somatostatin-positive inhibitory cells and to whisker-evoked cortical activity.
Lorenzo Gesuita 1, Anna Cavaccini 1, Ali Özgür Argunsah 1, Emilia Favuzzi 2, Leena Ali Ibrahim 2, Tevye Jason Stachniak 1, Martina De Gennaro 1, Sebastian Utz 3, Melanie Greter 3, Theofanis Karayannis 4
Immunity 2021 July 13, 54, 1–16.
Treg cell-derived osteopontin promotes microglia-mediated white matter repair after ischemic stroke.
Ligen Shi, Zeyu Sun, Wei Su, Fei Xu, Di Xie, and Xiaoming Hu
J Neuroinflammation. 2022; 19: 173.
Repopulated microglia induce expression of Cxcl13 with differential changes in Tau phosphorylation but do not impact amyloid pathology.
Berke Karaahmet,#1 Linh Le,#1 Monique S. Mendes,#1,2 Ania K. Majewska,corresponding author1 and M. Kerry O’Banioncorresponding author1
Nat Commun. 2019 Aug 21;10(1):3758.
Sustained microglial depletion with CSF1R inhibitor impairs parenchymal plaque development in an Alzheimer's disease model.
Disclaimer: For laboratory research use only.
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