PLX5622 hemifumarate
Based on 101 publication(s) in Google Scholar
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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.93%
- Fòrmula: C23H21F2N5O3
- Peso molecular:453.45
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Almacenamiento:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Publications Citing Use of MedChemExpress (MCE) PLX5622 hemifumarate
More- Signal Transduct Target Ther. 2026 Mar 25;11(1):109. [Abstract]
- Nature. 2026 Jun;654(8120):1033-1043. [Abstract]
- Nature. 2025 Jul;643(8071):509-518. [Abstract]
- Nature. 2021 Feb;590(7847):612-617. [Abstract]
- Cell. 2025 Apr 17;188(8):2159-2174.e15. [Abstract]
- Cell. 2023 Sep 28;186(20):4454-4471.e19. [Abstract]
- Immunity. 2024 Nov 12;57(11):2651-2668.e12. [Abstract]
- Nat Metab. 2025 Sep 23. [Abstract]
- Cell Stem Cell. 2025 Apr 3;32(4):652-669.e11. [Abstract]
- Nat Neurosci. 2026 Jul 16.
- Nat Neurosci. 2024 Aug;27(8):1468-1474. [Abstract]
- Nat Commun. 2025 Jul 1;16(1):5616. [Abstract]
- Nat Commun. 2024 Dec 6;15(1):10635. [Abstract]
- Nat Commun. 2023 Dec 13;14(1):8273. [Abstract]
- Neuron. 2026 Apr 15;114(8):1419-1432.e7. [Abstract]
- Redox Biol. 2025 Jul:84:103682. [Abstract]
- J Clin Invest. 2025 Aug 19:e184325. [Abstract]
- Adv Sci (Weinh). 2025 Mar;12(11):e2412556. [Abstract]
- Adv Sci (Weinh). 2025 Jan;12(4):e2410360. [Abstract]
- Sci Adv. 2026 Mar 13;12(11):eadz1686. [Abstract]
- Cell Death Differ. 2024 Aug;31(8):983-998. [Abstract]
- Brain. 2024 Jul 5;147(7):2384-2399. [Abstract]
- Nat Cardiovasc Res. 2022 Jul;1(7):649-664. [Abstract]
- Cell Mol Biol Lett. 2024 Aug 28;29(1):114. [Abstract]
- J Exp Med. 2023 Mar 6;220(3):e20220857. [Abstract]
- J Neuroinflammation. 2025 Jan 31;22(1):26. [Abstract]
- J Neuroinflammation. 2024 Apr 10;21(1):88. [Abstract]
- J Neuroinflammation. 2023 Nov 17;20(1):269. [Abstract]
- J Neuroinflammation. 2022 Dec 14;19(1):300. [Abstract]
- Mol Ther. 2025 Nov 12:S1525-0016(25)00872-X. [Abstract]
- Mol Ther. 2025 Nov 12:S1525-0016(25)00871-8. [Abstract]
- Stroke. 2026 Jul;57(7):2194-2207. [Abstract]
- Acta Pharmacol Sin. 2026 Jan 1. [Abstract]
- Mol Psychiatry. 2025 Aug 6. [Abstract]
- Cell Death Discov. 2023 Oct 21;9(1):388. [Abstract]
- Br J Anaesth. 2026 Jul;137(1):154-167. [Abstract]
- Basic Res Cardiol. 2022 Oct 24;117(1):52. [Abstract]
- Neural Regen Res. 2025 Jul 5. [Abstract]
- NPJ Parkinsons Dis. 2024 Feb 2;10(1):32. [Abstract]
- Free Radic Biol Med. 2024 Nov 20:225:469-481. [Abstract]
- Clin Transl Med. 2024 Apr;14(4):e1665. [Abstract]
- EMBO Mol Med. 2023 Feb 8;15(2):e17175. [Abstract]
- Cell Rep. 2023 Jun 6;42(6):112617. [Abstract]
- Cell Rep. 2020 Aug 11;32(6):108041. [Abstract]
- Brain Behav Immun. 2026 Jan 26:134:106472. [Abstract]
- Brain Behav Immun. 2026 Jan:131:106148. [Abstract]
- Brain Behav Immun. 2023 Nov:114:287-298. [Abstract]
- Fluids Barriers CNS. 2023 Jun 9;20(1):42. [Abstract]
- JCI Insight. 2025 Mar 6;10(8):e181885. [Abstract]
- JCI Insight. 2024 Feb 6;9(6):e175015. [Abstract]
- Acta Neuropathol Commun. 2026 May 13;14(1):144. [Abstract]
- Vis Neurosci. 2025 Mar 27.
- Neurobiol Dis. 2022 Nov 1;175:105914. [Abstract]
- Commun Biol. 2026 Mar 19. [Abstract]
- Eur J Pharmacol. 2025 Jun 5:996:177424. [Abstract]
- Int J Mol Sci. 2023 Nov 27;24(23):16803. [Abstract]
- Glia. 2021 Oct;69(10):2332-2348. [Abstract]
- Brain Commun. 2026 Jun 2;8(3):fcag202.
- iScience. 2023 Jul 3;26(8):107264. [Abstract]
- FASEB J. 2024 Jan 31;38(2):e23419. [Abstract]
- Chem Res Toxicol. 2026 Jun 27. [Abstract]
- Eur Arch Psychiatry Clin Neurosci. 2022 Apr;272(3):483-495. [Abstract]
- Brain Behav Immun Health. 2026 May 20:54:101264. [Abstract]
- Mol Pain. 2020 Jan-Dec:16:1744806920934998. [Abstract]
- Brain Res. 2026 Feb 1:1872:150107. [Abstract]
- IUBMB Life. 2024 Dec;76(12):1209-1222. [Abstract]
- NMR Biomed. 2024 Dec;37(12):e5222. [Abstract]
- PLoS One. 2022 Aug 18;17(8):e0269140. [Abstract]
- eNeuro. 2023 Nov 10;10(11):ENEURO.0323-23.2023. [Abstract]
- Curr Eye Res. 2026 Mar;51(3):276-284. [Abstract]
- STAR Protoc. 2021 Jul 9;2(3):100665. [Abstract]
- STAR Protoc. 2021 Jul 7;2(3):100666. [Abstract]
- STAR Protoc. 2021 Jun 11;2(2):100613. [Abstract]
- Vanderbilt University. 2026.
- LSU Health Shreveport. 2026.
- bioRxiv. 2026 Apr 28.
- bioRxiv. 2026 Apr 8:2026.04.06.716590. [Abstract]
- bioRxiv. 2026 Feb 23.
- Res Sq. 2026 Feb 10.
- bioRxiv. 2026 Jan 16:2026.01.15.699551. [Abstract]
- Res Sq. 2025 Dec 10:rs.3.rs-6323329. [Abstract]
- University of Regensburg. 2025 Dec 3.
- bioRxiv. 2025 Oct 9.
- SSRN. 2025 Oct 1.
- Patent. US20250241950A1.
- University of New Mexico. 2025 Jun 16.
- SSRN. 2025 Jun 18.
- Patent. US20250002920A1.
- Research Square Preprint. 2024 Dec 12.
- bioRxiv. 2024 Nov 4:2024.11.04.621917. [Abstract]
- bioRxiv. 2024 Aug 12:2024.08.12.607566. [Abstract]
- bioRxiv. 2024 July 02.
- bioRxiv. 2024 Apr 3:2023.11.16.567220. [Abstract]
- bioRxiv. 2023 Oct 28.
- Patent. US20230203500A1.
- The University of Texas at San Antonio. 2023 May.
- bioRxiv. 2023 May 3:2023.04.28.538637. [Abstract]
- Elife. 2021 Jun 23:10:e67772. [Abstract]
- Research Square Preprint. 2021 Mar.
- bioRxiv. 2021 Feb 26.
- bioRxiv. 2021 Feb 27.
Customer Validation & Images
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IF
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In Vivo Efficacy Study
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IF
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Flow Cytometry
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Bio/Physico-chemical Assay
Actividad biológica
Descripciòn
IC50 & Target
CSF1R[1]
In Vitro
PLX5622 (1-20 μM; 3 days) hemifumarate effectively depletes microglia without affecting oligodendrocytes or astrocytes in cerebellar slices. PLX5622 (4 μM; 3 days) hemifumarate causes a 30-40% reduction in NG2+ or PDGFRα+ cells, and this increased to 90-95% at 20 μM. No reduction of NG2+ or PDGFRα+ OPCs is observed in slices exposed to 1 μM or 2 μM PLX5622 despite robust (~95%) depletion of the microglial cells[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
PLX5622 (1200 ppm; chow; for 3 weeks or 3 days; adult C57/Bl6 wild type mice) hemifumarate leads to around 80% of microglia lost after 3 days of treatment and a 99% microglia loss after 3 weeks of treatment. PLX5622 (adult C57/Bl6 wild type mice aged 3 months; diet for 3 weeks) decreases microglia in cortex, striatum, cerebellum and hippocampus[4].
PLX5622 (50 mg/kg; intraperitoneal injection; once (neonatal rat) or twice (adult rat) a day; for a total of 14 days) hemifumarate depletes microglia by 80-90% within 3 days of treatment, which increases to > 90% by 7 days. After 14 days of PLX5622 treatment, microglia is depleted by > 96% in both neonates and adults while preserving baseline astrocyte quantity. (A single daily injection of 0.65% PLX5622 suspended in 5% dimethyl sulfoxide and 20% Kolliphor RH40 in 0.01 M PBS is sufficient for neonatal microglia depletion, adult depletion requires injections twice daily)[5].
PLX5622 (formulated in AIN-76A standard chow at 1200 mg/kg; for 28 days) hemifumarate leads to reduction in microglia throughout the CNS in 14-month-old 5xfAD mice[6].
Pharmacokinetics of PLX5622 hemifumarate in preclinical species[4]
| Species | IV | PO (gavage) | |||||||
| Dose (mg/kg) |
AUC0-∞ (ng hr/mL) |
CL (mL/min/kg) |
Vss (L/kg) |
t1/2 (hr) |
Dose (mg/kg) |
AUC0-∞ (ng hr/mL) |
Cmax (ng/mL) |
F | |
| Mouse | 1.92 | 15,500 | 2.1 | 0.34 | 2.6 | 45 | 215,000 | 26,300 | 59% |
| Rat (male) | 1.13 | 2,630 | 7.7 | 1.2 | 2.3 | 45 | 99,600 | 12,000 | 95% |
| Rat (female) | 1.13 | 5,110 | 3.7 | 1.0 | 3.9 | 45 | 181,000 | 15,600 | 89% |
| Dog | 1.00 | 6,230 | 3.0 | 2.3 | 15 | 45 | 96,500 | 3,630 | 34% |
| Monkey | 1.35 | 2,100 | 11 | 1.6 | 2.2 | ND | ND | ND | ND |
Preparation of gavage dosing suspensions for PLX5622 hemifumarate[4]
PLX5622 hemifumarate is dissolved in DMSO at a concentration that is 20x the final dosing solution. The compound stock is protected from light. A fresh stock is made each week.
The components of the diluent generally are prepared a day or more in advance because they take time to dissolve completely: a) 2% hydroxypropyl methyl cellulose (HPMC): 2.0 g powder was brought to 100 mL deionized water; b) 25% Polysorbate 80 (PS80): 25 g was brought to 100 mL deionized water. To make 100 mL diluent, add 25 mL of 2% HPMC stock (0.5% final) and 4 mL of 25% PS80 stock (1% final) to 71 mL deionized water to have final 100 mL. Final composition after mixing with compound: 0.5% HPMC, 1% PS80, 5% DMSO.
On each dosing day, the compound stock is diluted 20-fold as follows: 19 volumes of diluent are measured into the tube, and 1 volume of the 20x compound/DMSO stock is added. The cap is closed and the content of the tube is mixed by inversion and placed in a sonicating water bath to make a uniform suspension.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Pregnant CD1 dams[7]
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Dosage:1200 PPM
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Administration:Fed diet; from embryonic day 3.5 (E3.5) to embryonic day 15.5 (E15.5)
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Result:Once the treatment was removed, microglia repopulated the postnatal brain within 7 days and did not appear to repopulate from Nestin+ precursors.
Resulted in a decreased litter size, and an increase in the number of pups that died within the first two postnatal days of life.
Surviving exposed animals displayed craniofacial and dental abnormalities.
Depletion of microglia during embryogenesis had long-term sex-specific effects on behaviour, including the development of hyperactivity and anxiolytic-like behaviour in juvenile and adult female mice, respectively.
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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Appearance Solid
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Peso molecular 453.45
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Fòrmula C23H21F2N5O3
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Color Off-white to light yellow
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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
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (101)
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Journal Impact Factor
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Most Recent
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Signal Transduct Target Ther
Oligodendrocyte precursor cells-microglia crosstalk via BMP4 drives microglial neuroprotective response and mitigates Alzheimer's disease. [Abstract]2026 Mar 25;11(1):109. PMID: 41881962 -
Nature
2026 Jun;654(8120):1033-1043. PMID: 42020752 -
Nature
2025 Jul;643(8071):509-518. PMID: 40533562
PLX5622 hemifumarate purchased from MedChemExpress. Usage Cited in: Nature. 2025 Jul;643(8071):509-518. [Abstract]
PLX5622 (1200 ppm; Fed diet). IBA1-expressing microglia/macrophages in the brainstem of Rag2−/− recipients of CD4-tdTomato+ TCR7B8 CD4 T cells 6 to 7 weeks after transfer.
PLX5622 hemifumarate purchased from MedChemExpress. Usage Cited in: Nature. 2025 Jul;643(8071):509-518. [Abstract]
PLX5622 (1200 ppm; Fed diet). Neurological score of Csf2-deficient or Csf2-sufficient TCR7B8 transferred hosts with or without CSF1R inhibitor treatment.
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Nature
2021 Feb;590(7847):612-617. PMID: 33361813 -
Cell
Peripheral nervous system microglia-like cells regulate neuronal soma size throughout evolution. [Abstract]2025 Apr 17;188(8):2159-2174.e15. PMID: 40199320 -
Cell
An immune cell atlas reveals the dynamics of human macrophage specification during prenatal development. [Abstract]2023 Sep 28;186(20):4454-4471.e19. PMID: 37703875 -
Immunity
Apolipoprotein E aggregation in microglia initiates Alzheimer's disease pathology by seeding β-amyloidosis. [Abstract]2024 Nov 12;57(11):2651-2668.e12. PMID: 39419029
PLX5622 hemifumarate purchased from MedChemExpress. Usage Cited in: Immunity. 2024 Nov 12;57(11):2651-2668.e12. [Abstract]
PLX5622 (0.12%; Fed diet). Tile scan images and magnified images show MX04 (gray) labeling for plaque visualization in injected areas as well as IBA1 (magenta) and CD68 (cyan) staining.
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Nat Metab
Cholesterol metabolic reprogramming mediates microglia-induced chronic neuroinflammation and hinders neurorestoration following stroke. [Abstract]2025 Sep 23. PMID: 40987840
PLX5622 hemifumarate purchased from MedChemExpress. Usage Cited in: Nat Metab. 2025 Sep 23. [Abstract]
PLX5622 (1200 mg/kg; Fed diet). MBP immunostaining revealing enhanced white matter repair (reduced MBP+ area loss) in the striatum of PLX-treated MCAO mice compared to vehicle controls.
PLX5622 hemifumarate purchased from MedChemExpress. Usage Cited in: Nat Metab. 2025 Sep 23. [Abstract]
PLX5622 (1200 mg/kg; Fed diet). PLX treatment significantly depleted the microglial population following MCAO. n = 3 mice/group.
PLX5622 hemifumarate purchased from MedChemExpress. Usage Cited in: Nat Metab. 2025 Sep 23. [Abstract]
Efavirenz (EFV) (0.09 mg/kg; i.g.; once daily) treatment significantly downregulated pro-inflammatory transcripts of microglia in MCAO mice.
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Cell Stem Cell
Individualized patient tumor organoids faithfully preserve human brain tumor ecosystems and predict patient response to therapy. [Abstract]2025 Apr 3;32(4):652-669.e11. PMID: 39938519 -
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Nat Neurosci
T cell-mediated microglial activation triggers myelin pathology in a mouse model of amyloidosis. [Abstract]2024 Aug;27(8):1468-1474. PMID: 38937583 -
Nat Commun
2025 Jul 1;16(1):5616. PMID: 40595560 -
Nat Commun
Intratumoral delivery of lipid nanoparticle-formulated mRNA encoding IL-21, IL-7, and 4-1BBL induces systemic anti-tumor immunity. [Abstract]2024 Dec 6;15(1):10635. PMID: 39639025 -
Nat Commun
DPPIV+ fibro-adipogenic progenitors form the niche of adult skeletal muscle self-renewing resident macrophages. [Abstract]2023 Dec 13;14(1):8273. PMID: 38092736 -
Neuron
More than microglial depletion: PLX5622 activates the hepatic constitutive androstane receptor to alter anesthesia and addiction. [Abstract]2026 Apr 15;114(8):1419-1432.e7. PMID: 41734759 -
Redox Biol
Muscle-derived factor alleviated cognitive impairment caused by intestinal ischemia-reperfusion. [Abstract]2025 Jul:84:103682. PMID: 40388874 -
J Clin Invest
Hypertension promotes bone loss and fragility by favoring bone resorption in mouse models. [Abstract]2025 Aug 19:e184325. PMID: 40828611 -
Adv Sci (Weinh)
Microglia-Derived Interleukin-6 Triggers Astrocyte Apoptosis in the Hippocampus and Mediates Depression-Like Behavior. [Abstract]2025 Mar;12(11):e2412556. PMID: 39888279 -
Adv Sci (Weinh)
Targeted SPP1 Inhibition of Tumor-Associated Myeloid Cells Effectively Decreases Tumor Sizes. [Abstract]2025 Jan;12(4):e2410360. PMID: 39639496 -
Sci Adv
Persistent microglial activation following neonatal CMV infection mediates neurodegeneration. [Abstract]2026 Mar 13;12(11):eadz1686. PMID: 41811959 -
Cell Death Differ
2024 Aug;31(8):983-998. PMID: 38719928 -
Brain
A cell autonomous regulator of neuronal excitability modulates tau in Alzheimer's disease vulnerable neurons. [Abstract]2024 Jul 5;147(7):2384-2399. PMID: 38462574 -
Nat Cardiovasc Res
2022 Jul;1(7):649-664. PMID: 36034743 -
Cell Mol Biol Lett
Pterostilbene improves neurological dysfunction and neuroinflammation after ischaemic stroke via HDAC3/Nrf1-mediated microglial activation. [Abstract]2024 Aug 28;29(1):114. PMID: 39198723 -
J Exp Med
2023 Mar 6;220(3):e20220857. PMID: 36584406 -
J Neuroinflammation
Rescue of in vitro models of CSF1R-related adult-onset leukodystrophy by iluzanebart: mechanisms and therapeutic implications of TREM2 agonism. [Abstract]2025 Jan 31;22(1):26. PMID: 39891235 -
J Neuroinflammation
Fascin-1 limits myosin activity in microglia to control mechanical characterization of the injured spinal cord. [Abstract]2024 Apr 10;21(1):88. PMID: 38600569 -
J Neuroinflammation
Cytokine enrichment in deep cerebellar nuclei is contributed by multiple glial populations and linked to reduced amyloid plaque pathology. [Abstract]2023 Nov 17;20(1):269. PMID: 37978387 -
J Neuroinflammation
Models of microglia depletion and replenishment elicit protective effects to alleviate vascular and neuronal damage in the diabetic murine retina. [Abstract]2022 Dec 14;19(1):300. PMID: 36517889 -
Mol Ther
2025 Nov 12:S1525-0016(25)00872-X. PMID: 41232524 -
Mol Ther
Microglia replacement by peripheral delivery of CSF1R inhibitor-resistant hematopoietic cells. [Abstract]2025 Nov 12:S1525-0016(25)00871-8. PMID: 41232525 -
Stroke
Adiponectin Fortifies White Matter After Chronic Hypoperfusion-Induced Vascular Dementia. [Abstract]2026 Jul;57(7):2194-2207. PMID: 42131908 -
Acta Pharmacol Sin
NLRP3 facilitates α-synuclein-induced dopaminergic neuronal senescence in a mouse model of Parkinson's disease through SATB1/DNA damage/p21 signaling pathway. [Abstract]2026 Jan 1. PMID: 41476182 -
Mol Psychiatry
Anterior insular cortex regulates depression-like and ASD-like behaviors via the differential contribution of two subsets of microglia. [Abstract]2025 Aug 6. PMID: 40770435 -
Cell Death Discov
Dopaminergic neurodegeneration in the substantia nigra is associated with olfactory dysfunction in mice models of Parkinson's disease. [Abstract]2023 Oct 21;9(1):388. PMID: 37865662 -
Br J Anaesth
Microglial activation disrupts hippocampal CA1 sharp-wave ripples via the CA3-CA1 neural circuit that contributes to postoperative memory consolidation deficits in aged mice. [Abstract]2026 Jul;137(1):154-167. PMID: 42091343 -
Basic Res Cardiol
Molecular imaging of the brain-heart axis provides insights into cardiac dysfunction after cerebral ischemia. [Abstract]2022 Oct 24;117(1):52. PMID: 36279013 -
Neural Regen Res
Delayed microglial depletion protects against white matter injury following neonatal cerebral hemorrhage in mice. [Abstract]2025 Jul 5. PMID: 40618257 -
NPJ Parkinsons Dis
Microglial inhibition alleviates alpha-synuclein propagation and neurodegeneration in Parkinson's disease mouse model. [Abstract]2024 Feb 2;10(1):32. PMID: 38302446 -
Free Radic Biol Med
A critical role for microglia in regulating metabolic homeostasis and neural repair after spinal cord injury. [Abstract]2024 Nov 20:225:469-481. PMID: 39413980 -
Clin Transl Med
TREM2 alleviates white matter injury after traumatic brain injury in mice might be mediated by regulation of DHCR24/LXR pathway in microglia. [Abstract]2024 Apr;14(4):e1665. PMID: 38649789 -
EMBO Mol Med
2023 Feb 8;15(2):e17175. PMID: 36541061 -
Cell Rep
Resolvin D1 reprograms energy metabolism to promote microglia to phagocytize neutrophils after ischemic stroke. [Abstract]2023 Jun 6;42(6):112617. PMID: 37285269 -
Cell Rep
2020 Aug 11;32(6):108041. PMID: 32783928 -
Brain Behav Immun
Circulating Ly6Chigh monocyte-derived S100A4+ macrophages exacerbate neuroinflammation and impede recovery of traumatic brain injury. [Abstract]2026 Jan 26:134:106472. PMID: 41605306 -
Brain Behav Immun
Microglia-mediated Perineuronal nets loss contributes to social memory deficit in male mice after repeated neonatal sevoflurane exposure. [Abstract]2026 Jan:131:106148. PMID: 41138885 -
Brain Behav Immun
Microglia depletion ameliorates neuroinflammation, anxiety-like behavior, and cognitive deficits in a sex-specific manner in Rev-erbα knockout mice. [Abstract]2023 Nov:114:287-298. PMID: 37648007 -
Fluids Barriers CNS
Early postnatal microglial ablation in the Ccdc39 mouse model reveals adverse effects on brain development and in neonatal hydrocephalus. [Abstract]2023 Jun 9;20(1):42. PMID: 37296418 -
JCI Insight
MSC transplantation ameliorates depression in lupus by suppressing Th1 cell-shaped synaptic stripping. [Abstract]2025 Mar 6;10(8):e181885. PMID: 40048256 -
JCI Insight
2024 Feb 6;9(6):e175015. PMID: 38516884 -
Acta Neuropathol Commun
Age-dependent peripheral dissemination of α-synuclein seeds: mechanistic basis for blood-based early detection of Parkinson's disease. [Abstract]2026 May 13;14(1):144. PMID: 42129944 -
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Neurobiol Dis
The contribution of spinal dorsal horn astrocytes in neuropathic pain at the early stage of EAE. [Abstract]2022 Nov 1;175:105914. PMID: 36332813 -
Commun Biol
Astrocytic EAAT1 suppression by EV-ACLY underlies glutamate imbalance and cognitive impairment in POCD. [Abstract]2026 Mar 19. PMID: 41857316 -
Eur J Pharmacol
Arctiin attenuated NASH by inhibiting glycolysis and inflammation via FGFR2/CSF1R signaling. [Abstract]2025 Jun 5:996:177424. PMID: 40010483 -
Int J Mol Sci
CXCR2-Blocking Has Context-Sensitive Effects on Rat Glioblastoma Cell Line Outgrowth (S635) in an Organotypic Rat Brain Slice Culture Depending on Microglia-Depletion (PLX5622) and Dexamethasone Treatment. [Abstract]2023 Nov 27;24(23):16803. PMID: 38069130 -
Glia
Transnasal transplantation of human induced pluripotent stem cell-derived microglia to the brain of immunocompetent mice. [Abstract]2021 Oct;69(10):2332-2348. PMID: 34309082 -
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iScience
SnRNA-seq reveals the heterogeneity of spinal ventral horn and mechanism of motor neuron axon regeneration. [Abstract]2023 Jul 3;26(8):107264. PMID: 37502257 -
FASEB J
2024 Jan 31;38(2):e23419. PMID: 38236370 -
Chem Res Toxicol
Characterizing the Reactive Metabolites of Colony-Stimulating Factor 1 Receptor Inhibitor PLX5622 in Liver Microsomes and Mice. [Abstract]2026 Jun 27. PMID: 42363912 -
Eur Arch Psychiatry Clin Neurosci
Microglial depletion and abnormalities in gut microbiota composition and short-chain fatty acids in mice after repeated administration of colony stimulating factor 1 receptor inhibitor PLX5622. [Abstract]2022 Apr;272(3):483-495. PMID: 34480631 -
Brain Behav Immun Health
Microglia depletion alleviates the disruptions in circadian rhythms and anxiety caused by bmal1 deficiency. [Abstract]2026 May 20:54:101264. PMID: 42210978 -
Mol Pain
2020 Jan-Dec:16:1744806920934998. PMID: 32580615 -
Brain Res
Astrocyte regulates neuroinflammation and myelination in BCCAO-related cognitive impairment via the PIAS1-STAT1 pathway. [Abstract]2026 Feb 1:1872:150107. PMID: 41380753 -
IUBMB Life
Microglia synchronizes with the circadian rhythm of the glymphatic system and modulates glymphatic system function. [Abstract]2024 Dec;76(12):1209-1222. PMID: 39223969 -
NMR Biomed
Brain volume and microglial density changes are correlated in a juvenile mouse model of cranial radiation and CSF1R inhibitor treatment. [Abstract]2024 Dec;37(12):e5222. PMID: 39164196 -
PLoS One
2022 Aug 18;17(8):e0269140. PMID: 35980963 -
eNeuro
2023 Nov 10;10(11):ENEURO.0323-23.2023. PMID: 37890992 -
Curr Eye Res
2026 Mar;51(3):276-284. PMID: 41566967 -
STAR Protoc
2021 Jul 9;2(3):100665. PMID: 34308380 -
STAR Protoc
Microglia replacement by bone marrow transplantation (Mr BMT) in the central nervous system of adult mice. [Abstract]2021 Jul 7;2(3):100666. PMID: 34286294 -
STAR Protoc
2021 Jun 11;2(2):100613. PMID: 34179837 -
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bioRxiv
2026 Apr 8:2026.04.06.716590. PMID: 41993267 -
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bioRxiv
Microglial epigenetic memory is associated with accelerated resolution of inflammatory pain induced by prophylactic macrophage-derived small extracellular vesicles. [Abstract]2026 Jan 16:2026.01.15.699551. PMID: 41648229 -
Res Sq
Erythrocyte-microglia crosstalk contributing to sex differences in pediatric brain tumorigenesis. [Abstract]2025 Dec 10:rs.3.rs-6323329. PMID: 41510281 -
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bioRxiv
Pharmacological depletion of microglia protects against alcohol-induced corticolimbic neurodegeneration during intoxication in male rats. [Abstract]2024 Nov 4:2024.11.04.621917. PMID: 39574620 -
bioRxiv
Microglia are Required for Developmental Specification of AgRP Innervation in the Hypothalamus of Offspring Exposed to Maternal High Fat Diet During Lactation. [Abstract]2024 Aug 12:2024.08.12.607566. PMID: 39185162 -
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bioRxiv
Dynamic neuroinflammatory profiles predict Alzheimer's disease pathology in microglia-containing cerebral organoids. [Abstract]2024 Apr 3:2023.11.16.567220. PMID: 38014053 -
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bioRxiv
Chimeric Antigen Receptor Macrophages Target and Resorb Amyloid Plaques in a Mouse Model of Alzheimer's Disease. [Abstract]2023 May 3:2023.04.28.538637. PMID: 37162824 -
Elife
Dual targeting of salt inducible kinases and CSF1R uncouples bone formation and bone resorption. [Abstract]2021 Jun 23:10:e67772. PMID: 34160349 -
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Solvente y solubilidad
In Vitro:
DMSO : 110 mg/mL (242.58 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 3.25 mg/mL (7.17 mM); Clear solution
This protocol yields a clear solution of ≥ 3.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (32.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 3.25 mg/mL (7.17 mM); Clear solution
This protocol yields a clear solution of ≥ 3.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (32.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (302 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
[4]. Badimon A, et al. Negative feedback control of neuronal activity by microglia. Nature. 2020;586(7829):417-423. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2053 mL | 11.0266 mL | 22.0531 mL | 55.1329 mL |
| 5 mM | 0.4411 mL | 2.2053 mL | 4.4106 mL | 11.0266 mL | |
| 10 mM | 0.2205 mL | 1.1027 mL | 2.2053 mL | 5.5133 mL | |
| 15 mM | 0.1470 mL | 0.7351 mL | 1.4702 mL | 3.6755 mL | |
| 20 mM | 0.1103 mL | 0.5513 mL | 1.1027 mL | 2.7566 mL | |
| 25 mM | 0.0882 mL | 0.4411 mL | 0.8821 mL | 2.2053 mL | |
| 30 mM | 0.0735 mL | 0.3676 mL | 0.7351 mL | 1.8378 mL | |
| 40 mM | 0.0551 mL | 0.2757 mL | 0.5513 mL | 1.3783 mL | |
| 50 mM | 0.0441 mL | 0.2205 mL | 0.4411 mL | 1.1027 mL | |
| 60 mM | 0.0368 mL | 0.1838 mL | 0.3676 mL | 0.9189 mL | |
| 80 mM | 0.0276 mL | 0.1378 mL | 0.2757 mL | 0.6892 mL | |
| 100 mM | 0.0221 mL | 0.1103 mL | 0.2205 mL | 0.5513 mL |
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