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PLX5622 (hemifumarate)

PLX5622 hemifumarate is a highly selective brain penetrant and orally active CSF1R inhibitor (IC50=0.016 μM; Ki=5.9 nM) . PLX5622 hemifumarate allows for extended and specific microglial elimination, preceding and during pathology development. PLX5622 hemifumarate demonstrates desirable PK properties in varies animals[1][2].

Product Specifications

Product Name Alternative

GCA

UNSPSC

12352005

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-hemifumarate.html

Concentration

10mM

Purity

99.93

Solubility

DMSO : 110 mg/mL (ultrasonic)

Smiles

COC1=NC=C(F)C=C1CNC2=NC(F)=C(CC3=CNC4=NC=C(C)C=C43)C=C2.O=C(O)/C=C/C(O)=O

Molecular Formula

C23H21F2N5O3

Molecular Weight

453.45

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]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.|[4]Badimon A, et al. Negative feedback control of neuronal activity by microglia. Nature. 2020;586 (7829) :417-423.|[5]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.|[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

4°C (Powder, sealed storage, away from moisture)

Scientific Category

Reference compound1

Clinical Information

Phase 1

Citation 01

BioRxiv. 2024 Aug 12:2024.08.12.607566.|Nat Commun. 2023 Dec 13;14 (1) :8273.|Redox Biol. 2025 May 15:84:103682.|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.

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