PLX5622

Name: PLX5622
Brand: MedChemExpress
SKU: HY-114153
Rating: 5.0 (89 reviews)

Cat. No.: HY-114153 Purity: 99.79%: Data Sheet
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PLX5622

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

For research use only. We do not sell to patients.

CAS No. : 1303420-67-8

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	In-stock	Estimated Time of Arrival: December 31
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
500 mg	In-stock	Estimated Time of Arrival: December 31
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5 g	Get quote

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Customer Review

Based on 89 publication(s) in Google Scholar

Other Forms of PLX5622:

PLX5622 hemifumarate In-stock

89 Publications Citing Use of MCE PLX5622

In Vivo Efficacy Study

Flow Cytometry

Bio/Physico-chemical Assay

: PLX5622 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 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.

: PLX5622 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 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 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.

: PLX5622 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.

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Biological Activity
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References
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Description

IC₅₀ & Target

IC50: 0.016 μM (CSF1R); Ki: 5.9 nM (CSF1R)^[1]^[2]

In Vitro

PLX5622 (1-20 μM; 3 days) effectively depletes microglia without affecting oligodendrocytes or astrocytes in cerebellar slices. PLX5622 (4 μM; 3 days) 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.

Parmacokinetics

Species	Dose	Route	AUC	Clearance (CL)	V_d	T_1/2	Plasma Concentration	Bioavailability
Cynomolgus Monkey^[1]	1.35 mg/kg	i.v.	2,100 ng·h/mL	11 mL/min/kg	1.6 L/kg	2.2 h	/	/
Dog^[1]	1 mg/kg	i.v.	6,230 ng·h/mL	3 mL/min/kg	2.3 L/kg	15 h	/	/
Dog^[1]	45 mg/kg	p.o.	96,500 ng·h/mL	/	/	/	3,630 ng/mL	34%
Mice^[1]	1.92 mg/kg	i.v.	15,500 ng·h/mL	2.1 mL/min/kg	0.34 L/kg	2.6 h	/	/
Mice^[1]	45 mg/kg	p.o.	215,000 ng·h/mL	/	/	/	26,300 ng/mL	59%
Rat^[1]	1.13 (female) mg/kg	i.v.	5,110 ng·h/mL	3.7 mL/min/kg	1 L/kg	3.9 h	/	/
Rat^[1]	1.13 (male) mg/kg	i.v.	2,630 ng·h/mL	7.7 mL/min/kg	0.34 L/kg	2.3 h	/	/
Rat^[1]	45 (female) mg/kg	p.o.	181,000 ng·h/mL	/	/	/	15,600 ng/mL	89%
Rat^[1]	45 (male) mg/kg	p.o.	99,600 ng·h/mL	/	/	/	12,000 ng/mL	95%

In Vivo

Pharmacodynamics of PLX5622 in preclinical studies
PLX5622 (1200 ppm; chow; for 3 weeks or 3 days; adult C57/Bl6 wild type mice) 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) 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) leads to reduction in microglia throughout the CNS in 14-month-old 5xfAD mice^[6].
PLX5622 (1200 PPM in AIN-76A standard diet for 12 days) in CD1 pregnant dams eliminated approximately 99% of microglia from the embryonic brain from embryonic day 3.5 (E3.5) to embryonic day 15.5 (E15.5), and increased apoptotic cell numbers were observed in the developing hypothalamus^[7].

Preparation of gavage dosing suspensions for PLX5622^[1]
PLX5622 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.

Molecular Weight

395.41

Formula

C₂₁H₁₉F₂N₅O

CAS No.

1303420-67-8

Appearance

Solid

Color

White to yellow

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL (126.45 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Ethanol : 3.33 mg/mL (8.42 mM; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.5290 mL	12.6451 mL	25.2902 mL
5 mM	0.5058 mL	2.5290 mL	5.0580 mL
10 mM	0.2529 mL	1.2645 mL	2.5290 mL

View the 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Molarity Calculator
Dilution Calculator

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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.

Protocol 1

Add each solvent one by one: 5% DMSO 95% (0.5% HPMC/1% Tween-80 in water)
Solubility: 6.5 mg/mL (16.44 mM); Suspended solution; Need ultrasonic and warming
Protocol 2

Add each solvent one by one: 5% DMSO 95% (20% Ethoxylated hydrogenated castor oil in Saline)
Solubility: 5 mg/mL (12.65 mM); Clear solution; Need ultrasonic
Protocol 3

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 3.12 mg/mL (7.89 mM); Clear solution

This protocol yields a clear solution of ≥ 3.12 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (31.2 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.
Protocol 4

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.32 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Protocol 5

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (6.32 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

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

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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.

Purity & Documentation

Purity: 99.95%

Select Batch:

Data Sheet (283 KB) SDS (393 KB)

COA (250 KB) HNMR (361 KB) LCMS (110 KB) Elemental Analysis Report (108 KB)

Handling Instructions (2659 KB)

References

[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]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

Ethanol / DMSO	1 mM	2.5290 mL	12.6451 mL	25.2902 mL	63.2255 mL
Ethanol / DMSO	5 mM	0.5058 mL	2.5290 mL	5.0580 mL	12.6451 mL
DMSO	10 mM	0.2529 mL	1.2645 mL	2.5290 mL	6.3226 mL
	15 mM	0.1686 mL	0.8430 mL	1.6860 mL	4.2150 mL
	20 mM	0.1265 mL	0.6323 mL	1.2645 mL	3.1613 mL
	25 mM	0.1012 mL	0.5058 mL	1.0116 mL	2.5290 mL
	30 mM	0.0843 mL	0.4215 mL	0.8430 mL	2.1075 mL
	40 mM	0.0632 mL	0.3161 mL	0.6323 mL	1.5806 mL
	50 mM	0.0506 mL	0.2529 mL	0.5058 mL	1.2645 mL
	60 mM	0.0422 mL	0.2108 mL	0.4215 mL	1.0538 mL
	80 mM	0.0316 mL	0.1581 mL	0.3161 mL	0.7903 mL
	100 mM	0.0253 mL	0.1265 mL	0.2529 mL	0.6323 mL

PLX5622 Related Classifications

Neurological Disease

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PLX56221303420-67-8PLX 5622PLX-5622c-FmsCSF-1 receptorcolony stimulating factor 1 receptorCSF-1RCSF1RbrainpenetrantorallymicroglialeliminationprecedingpathologyInhibitorinhibitorinhibit

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PLX5622

Customer Review

Other Forms of PLX5622:

PLX5622 Related Antibodies

89 Publications Citing Use of MCE PLX5622

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Biological Activity

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References

Customer Review

PLX5622 Related Antibodies

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Complete Stock Solution Preparation Table

PLX5622 Related Classifications

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