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  5. 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.

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PLX5622 Chemical Structure

PLX5622 Chemical Structure

CAS No. : 1303420-67-8

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10 mM * 1 mL in DMSO
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Customer Review

Based on 48 publication(s) in Google Scholar

Other Forms of PLX5622:

PLX5622 Related Antibodies

Top Publications Citing Use of Products

48 Publications Citing Use of MCE PLX5622

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1][2].

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.

PLX5622 Related Antibodies
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].

Pharmacokinetics of PLX5622 in preclinical species[1]

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[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.
Clinical Trial
Molecular Weight

395.41

Formula

C21H19F2N5O
CAS No.
Appearance

Solid

Color

White to light 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 6 months
-20°C 1 month
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)

H2O : < 0.1 mg/mL (insoluble)

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

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

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%

SDS (393 KB)

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

Handling Instructions (2659 KB)
References

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. 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
Ethanol / DMSO 1 mM 2.5290 mL 12.6451 mL 25.2902 mL 63.2255 mL
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
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PLX5622 Related Classifications

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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