Art. -Nr.: HY-114153A

PLX5622 hemifumarate

98 Cited Publications

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Based on 98 publication(s) in Google Scholar

PLX5622 hemifumarate is a highly selective brain penetrant and orally active CSF1R inhibitor (IC₅₀=0.016 μM; K_i=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.

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Reinheit: 99.93%
Formel: C₂₃H₂₁F₂N₅O₃
Molecular Weight:453.45

Speicherung:

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

PLX5622 hemifumarate Chemical Structure

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Use of MCE Products

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (98)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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

Pharmacodynamics of PLX5622 hemifumarate in preclinical studies
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)
Species	Dose (mg/kg)	AUC_0-∞ (ng hr/mL)	CL (mL/min/kg)	Vss (L/kg)	t_1/2 (hr)	Dose (mg/kg)	AUC_0-∞ (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.

Animal Model:

Pregnant CD1 dams^[7]
Dosage:

1200 PPM
Administration:

Fed diet; from embryonic day 3.5 (E3.5) to embryonic day 15.5 (E15.5)
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.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

Appearance Solid
Molecular Weight 453.45
Formel C₂₃H₂₁F₂N₅O₃
Color Off-white to light yellow
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
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Publications (98)

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Journal Impact Factor

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

Focal white matter lesions drive grey matter inflammation and synapse loss. [Abstract]

2026 Jun;654(8120):1033-1043. PMID: 42020752
Nature

Gut inflammation promotes microbiota-specific CD4 T cell-mediated neuroinflammation. [Abstract]

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⁺ TCR^7B8 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 TCR^7B8 transferred hosts with or without CSF1R inhibitor treatment.
Nature

Astrocytes phagocytose adult hippocampal synapses for circuit homeostasis. [Abstract]

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 Oct 9:S1074-7613(24)00458-8. PMID: 39419029

PLX5622 hemifumarate purchased from MedChemExpress. Usage Cited in: Immunity. 2024 Oct 9:S1074-7613(24)00458-8. [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.
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.
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
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

Exploitable mechanisms of antibody and CAR mediated macrophage cytotoxicity. [Abstract]

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
Cell Death Differ

Itaconate protects ferroptotic neurons by alkylating GPx4 post stroke. [Abstract]

2024 May 8. PMID: 38719928
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
Adv Sci (Weinh)

Microglia-Derived Interleukin-6 Triggers Astrocyte Apoptosis in the Hippocampus and Mediates Depression-Like Behavior. [Abstract]

2025 Jan 30:e2412556. PMID: 39888279
Adv Sci (Weinh)

Targeted SPP1 Inhibition of Tumor-Associated Myeloid Cells Effectively Decreases Tumor Sizes. [Abstract]

2024 Dec 5:e2410360. PMID: 39639496
J Clin Invest

Hypertension promotes bone loss and fragility by favoring bone resorption in mouse models. [Abstract]

2025 Aug 19:e184325. PMID: 40828611
Sci Adv

Persistent microglial activation following neonatal CMV infection mediates neurodegeneration. [Abstract]

2026 Mar 13;12(11):eadz1686. PMID: 41811959
Mol Ther

Microglia replacement by peripheral delivery of CSF1R inhibitor-resistant hematopoietic cells. [Abstract]

2025 Nov 12:S1525-0016(25)00871-8. PMID: 41232525
Mol Ther

CSF1R inhibitor-resistant model for CNS-wide microglia replacement strategies. [Abstract]

2025 Nov 12:S1525-0016(25)00872-X. PMID: 41232524
Redox Biol

Muscle-derived factor alleviated cognitive impairment caused by intestinal ischemia-reperfusion. [Abstract]

2025 May 15:84:103682. PMID: 40388874
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

Neutrophils incite and macrophages avert electrical storm after myocardial infarction. [Abstract]

2022 Jul;1(7):649-664. PMID: 36034743
J Exp Med

Engineering an inhibitor-resistant human CSF1R variant for microglia replacement. [Abstract]

2023 Mar 6;220(3):e20220857. PMID: 36584406
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
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
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
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
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
EMBO Mol Med

Aged lipid-laden microglia display impaired responses to stroke. [Abstract]

2023 Feb 8;15(2):e17175. PMID: 36541061
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
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
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
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]

2025 Oct 23:131:106148. 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
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
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

Efficient Strategies for Microglia Replacement in the Central Nervous System. [Abstract]

2020 Aug 11;32(6):108041. PMID: 32783928
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
Neural Regen Res

Delayed microglial depletion protects against white matter injury following neonatal cerebral hemorrhage in mice. [Abstract]

2025 Jul 5. PMID: 40618257
Elife

Dual targeting of salt inducible kinases and CSF1R uncouples bone formation and bone resorption. [Abstract]

2021 Jun 23:10:e67772. PMID: 34160349
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

Chimeric antigen receptor macrophages target and resorb amyloid plaques. [Abstract]

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
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
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
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
Eur J Pharmacol

Arctiin attenuated NASH by inhibiting glycolysis and inflammation via FGFR2/CSF1R signaling. [Abstract]

2025 Jun 5:996:177424. PMID: 40010483
FASEB J

Microglia contribute to mammary tumor-induced neuroinflammation in a female mouse model. [Abstract]

2024 Jan 31;38(2):e23419. PMID: 38236370
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
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
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
Mol Pain

Microglia-mediated chronic psoriatic itch induced by imiquimod. [Abstract]

2020 Jan-Dec:16:1744806920934998. PMID: 32580615
NMR Biomed

Brain volume and microglial density changes are correlated in a juvenile mouse model of cranial radiation and CSF1R inhibitor treatment. [Abstract]

2024 Aug 20:e5222. PMID: 39164196
eNeuro

Microglia are dispensable for developmental dendrite pruning of mitral cells in mice. [Abstract]

2023 Nov 10;10(11):ENEURO.0323-23.2023. PMID: 37890992
Brain Res

Astrocyte regulates neuroinflammation and myelination in BCCAO-related cognitive impairment via the PIAS1-STAT1 pathway. [Abstract]

2025 Dec 9:1872:150107. PMID: 41380753
PLoS One

Acyloxyacyl hydrolase regulates microglia-mediated pelvic pain. [Abstract]

2022 Aug 18;17(8):e0269140. PMID: 35980963
Vis Neurosci

2025 Mar 27.
Curr Eye Res

Microglia and Retinal Vascularity: A Deeper Dive into Branching Dynamics. [Abstract]

2026 Mar;51(3):276-284. PMID: 41566967
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

Microglia replacement by microglia transplantation (Mr MT) in the adult mouse brain. [Abstract]

2021 Jul 9;2(3):100665. PMID: 34308380
STAR Protoc

Protocol for microglia replacement by peripheral blood (Mr PB). [Abstract]

2021 Jun 11;2(2):100613. PMID: 34179837
LSU Health Shreveport

2026.
bioRxiv

Viral Microglia Reprogramming Clears Oligomeric Neurotoxic Debris. [Abstract]

2026 Apr 8:2026.04.06.716590. PMID: 41993267
bioRxiv

2026 Apr 28.
Res Sq

2026 Feb 10.
bioRxiv

2026 Feb 23.
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
University of Regensburg

2025 Dec 3.
SSRN

2025 Oct 1.
bioRxiv

2025 Oct 9.
Patent

US20250241950A1.
University of New Mexico

2025 Jun 16.
SSRN

2025 Jun 18.
Patent

US20250002920A1.
Research Square Preprint

2024 Dec 12.
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
bioRxiv

2024 July 02.
bioRxiv

Dynamic neuroinflammatory profiles predict Alzheimer's disease pathology in microglia-containing cerebral organoids. [Abstract]

2024 Apr 3:2023.11.16.567220. PMID: 38014053
bioRxiv

2023 Oct 28.
Patent

US20230203500A1.
The University of Texas at San Antonio

2023 May.
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
Research Square Preprint

2021 Mar.
bioRxiv

2021 Feb 26.
bioRxiv

2021 Feb 27.

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.2053 mL

11.0266 mL

22.0531 mL

5 mM

0.4411 mL

2.2053 mL

4.4106 mL

10 mM

0.2205 mL

1.1027 mL

2.2053 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 3.25 mg/mL (7.17 mM); Clear solution

This protocol yields a clear solution of ≥ 3.25 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (32.5 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (289 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

[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. [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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

PLX5622 hemifumarate

98 Cited Publications

100 mg Angebot einholen

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PLX5622 hemifumarate

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

CNS-Penetrant Compound Library

Orally Active Compound Library

Targeted Diversity Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Highly Selective Inhibitors Library

Cytokine Inhibitors Library

Macrophage Related Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Clinical Compound Library Plus

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) PLX5622 hemifumarate

Biologische Aktivität

Chemical Information

Publications (98)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

PLX5622 hemifumarate

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

CNS-Penetrant Compound Library

Orally Active Compound Library

Targeted Diversity Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Highly Selective Inhibitors Library

Cytokine Inhibitors Library

Macrophage Related Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Clinical Compound Library Plus

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) PLX5622 hemifumarate

Biologische Aktivität

Chemical Information

Publications (98)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

PLX5622 hemifumarate Related Classifications

HY-114153A Related Classifications