PLX5622
PLX5622 is a highly selective brain penetrant and orally active CSF1R inhibitor (IC50=0.016 μM; Ki=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. PLX5622 is predominantly administered via ad libitum diets with a dose of 1200 ppm[1][2].
Product Specifications
CAS Number
[1303420-67-8]
UNSPSC
12352005
Hazard Statement
H302, H315, H319, H335
Target
C-Fms
Type
Reference compound
Related Pathways
Protein Tyrosine Kinase/RTK
Applications
Neuroscience-Neuromodulation
Field of Research
Neurological Disease
Assay Protocol
https://www.medchemexpress.com/plx5622.html
Purity
99.95
Solubility
DMSO : 50 mg/mL (ultrasonic) |Ethanol : 3.33 mg/mL (ultrasonic; warming; heat to 60°C)
Smiles
COC1=NC=C(F)C=C1CNC2=NC(F)=C(CC3=CNC4=NC=C(C)C=C43)C=C2
Molecular Formula
C21H19F2N5O
Molecular Weight
395.41
Precautions
H302, H315, H319, H335
References & Citations
[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.|[3]Badimon A, et al. Negative feedback control of neuronal activity by microglia. Nature. 2020;586 (7829) :417-423.|[4]Andrew J. Riquier, et al. Astrocytic response to neural injury is larger during development than in adulthood and is not predicated upon the presence of microglia, Brain, Behavior, & Immunity-Health, Volume 1, 2020, 100010, ISSN 2666-3546.|[5]Liu Y, et al. Concentration-dependent effects of CSF1R inhibitors on oligodendrocyte progenitor cells ex vivo and in vivo. Exp Neurol. 2019;318:32-41.|[6]Spangenberg EE, et al. Eliminating microglia in Alzheimer's mice prevents neuronal loss without modulating amyloid-β pathology. Brain. 2016;139 (Pt 4) :1265-1281.|[7]Rosin JM, et al. 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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Phase 1
Citation 01
Adv Sci (Weinh) . 2024 Dec 5:e2410360.|Adv Sci (Weinh) . 2025 Jan 30:e2412556.|Basic Res Cardiol. 2022 Oct 24;117 (1) :52.|bioRxiv. 2021 Feb 26.|bioRxiv. 2021 Feb 27.|bioRxiv. 2023 May 3:2023.04.28.538637.|bioRxiv. 2023 Oct 28.|bioRxiv. 2024 Apr 3:2023.11.16.567220.|bioRxiv. 2024 July 02.|bioRxiv. 2024 Nov 4:2024.11.04.621917.|bioRxiv. 2025 Oct 9.|Brain Behav Immun. 2023 Nov:114:287-298.|Brain Behav Immun. 2025 Oct 23:131:106148.|Brain. 2024 Jul 5;147 (7) :2384-2399.|Cell Death Differ. 2024 May 8.|Cell Death Discov. 2023 Oct 21;9 (1) :388.|Cell Mol Biol Lett. 2024 Aug 28;29 (1) :114.|Cell Rep. 2020 Aug 11;32 (6) :108041.|Cell Rep. 2023 Jun 6;42 (6) :112617.|Cell Stem Cell. 2025 Apr 3;32 (4) :652-669.e11.|Cell. 2023 Sep 28;186 (20) :4454-4471.e19.|Cell. 2025 Apr 17;188 (8) :2159-2174.e15.|Clin Transl Med. 2024 Apr;14 (4) :e1665.|Elife. 2021 Jun 23:10:e67772.|EMBO Mol Med. 2023 Feb 8;15 (2) :e17175.|eNeuro. 2023 Nov 10;10 (11) :ENEURO.0323-23.2023.|Eur Arch Psychiatry Clin Neurosci. 2022 Apr;272 (3) :483-495.|Eur J Pharmacol. 2025 Jun 5:996:177424.|FASEB J. 2024 Jan 31;38 (2) :e23419.|Fluids Barriers CNS. 2023 Jun 9;20 (1) :42.|Free Radic Biol Med. 2024 Nov 20.|Glia. 2021 Oct;69 (10) :2332-2348.|Immunity. 2024 Oct 9:S1074-7613 (24) 00458-8.|Int J Mol Sci. 2023 Nov 27;24 (23) :16803.|iScience. 2023 Jul 3;26 (8) :107264.|IUBMB Life. 2024 Dec;76 (12) :1209-1222.|J Clin Invest. 2025 Aug 19:e184325.|J Exp Med. 2023 Mar 6;220 (3) :e20220857.|J Neuroinflammation. 2022 Dec 14;19 (1) :300.|J Neuroinflammation. 2023 Nov 17;20 (1) :269.|J Neuroinflammation. 2024 Apr 10;21 (1) :88.|J Neuroinflammation. 2025 Jan 31;22 (1) :26.|JCI Insight. 2024 Feb 6;9 (6) :e175015.|JCI Insight. 2025 Mar 6;10 (8) :e181885.|Mol Pain. 2020 Jan-Dec:16:1744806920934998.|Mol Psychiatry. 2025 Aug 6.|Mol Ther. 2025 Nov 12.|Mol Ther. 2025 Nov 12:S1525-0016 (25) 00872-X.|Nat Cardiovasc Res. 2022 Jul;1 (7) :649-664.|Nat Commun. 2024 Dec 6;15 (1) :10635.|Nat Commun. 2025 Jul 1;16 (1) :5616.|Nat Metab. 2025 Sep 23.|Nat Neurosci. 2024 Aug;27 (8) :1468-1474.|Nature. 2021 Feb;590 (7847) :612-617.|Nature. 2025 Jul;643 (8071) :509-518.|Neural Regen Res. 2025 Jul 5.|Neurobiol Dis. 2022 Nov 1;175:105914.|NMR Biomed. 2024 Aug 20:e5222.|NPJ Parkinsons Dis. 2024 Feb 2;10 (1) :32.|Patent. US20230203500A1.|Patent. US20250002920A1.|Patent. US20250241950A1.|PLoS One. 2022 Aug 18;17 (8) :e0269140.|Research Square Preprint. 2021 Mar.|Research Square Preprint. 2024 Dec 12.|SSRN. 2025 Jun 18.|SSRN. 2025 Oct 1.|STAR Protoc. 2021 Jul 7;2 (3) :100666.|STAR Protoc. 2021 Jul 9;2 (3) :100665.|STAR Protoc. 2021 Jun 11;2 (2) :100613.|The University of Texas at San Antonio. 2023 May.|University of New Mexico. 2025 Jun 16.|Vis Neurosci. 2025 Mar 27.|bioRxiv. 2024 Aug 12:2024.08.12.607566.|Nat Commun. 2023 Dec 13;14 (1) :8273.|Redox Biol. 2025 May 15:84:103682.
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