PLX5622 |
Catalog No.GC36940
One-Click Copy Product Info
|
PLX5622 is a selective inhibitor of colony-stimulating factor 1 receptor (CSFR1) with an IC50 value of 0.016μM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1303420-67-8
Sample solution is provided at 25 µL, 10mM.
_1-3.$$$39978408@51.jpg');)
_1-9.$$$38538795@65.jpg');)
_1-9.$$$39112701@51.jpg');)
_1-7.$$$37316672@70.jpg');)
_366-372.$$$36198801@70.jpg');)
.$$$38565142@65.jpg');)
_1867-1883.$$$33248023@67.jpg');)
_eads6055.$$$39977546@45.jpg');)
_eadm9805.$$$40080571@45.jpg');)
_eadj3020.$$$39666821@45.jpg');)
_1-20.$$$39757301@28.jpg');)
_1-24.$$$38898113@28.jpg');)
_273-287.$$$36806353@46.jpg');)
_1-16.$$$37156877@44.jpg');)
_1-19.$$$37460805@44.jpg');)
_1291-1307.$$$34518654@46.jpg');)
PLX5622 is a selective inhibitor of colony-stimulating factor 1 receptor (CSFR1) with an IC50 value of 0.016μM[1]. PLX5622 mainly acts on microglia in the central nervous system[2].[2]. By inhibiting CSFR1, PLX5662 selectively depletes microglia without affecting other types of myeloid cells[2]. PLX5662 has been investigated as a tool to study the role of microglia in neurodegenerative diseases[2].
In vitro, primary mixed mouse astrocytes and microglia cells were extracted[3]. Cells were treated with 10 μM PLX5622 (Dilute with 20mM DMSO stock solution), where other control cells were treated with DMSO only[3]. After treating microglial cells with 10μM PLX5622, cell number starting im-mediately after cell extraction was reduced to 8% of the control group, and cell number starting at day in vitro 12 was further reduced to 25% of the control group[3]. After 4 weeks treatment, number of microglial decreased to 2%, then dropped to less than 0.5% after 6 weeks[3]. PLX5622 significantly inhibited the growth of microglia.
In vivo, C57BL/6NCrl mice were fed a diet with PLX5622 at 1200 mg/kg, while control groups were fed a diet with AIN76 at the same concentration[4]. After 5 months, a 95% reduction of microglia was observed in mice[4]. Resident macrophages in multiple organs were depleted, including colon (92.4%); adipose tissue (58.2%); lung (26.3%) and peritoneal cavity (90.2%)[4]. However, a recovery of microglia has been observed after removal of PLX5622[4]. The same repopulation was also shown in bone marrow and spleen, indicating that immune cells could revert after withdrawal of PLX5622[4].
References:
[1]Guenoun D, Blaise N, Sellam A, Roupret‐Serzec J, Jacquens A, Steenwinckel JV, Gressens P, Bokobza C. Microglial Depletion, a New Tool in Neuroinflammatory Disorders: Comparison of Pharmacological Inhibitors of the CSF‐1R. Glia. 2024 Dec 24.
[2]Spangenberg E, Severson PL, Hohsfield LA, Crapser J, Zhang J, Burton EA, Zhang Y, Spevak W, Lin J, Phan NY, Habets G. Sustained microglial depletion with CSF1R inhibitor impairs parenchymal plaque development in an Alzheimer’s disease model. Nature communications. 2019 Aug 21;10(1):3758.
[3]Hupp S, Iliev AI. CSF-1 receptor inhibition as a highly effective tool for depletion of microglia in mixed glial cultures. Journal of neuroscience methods. 2020 Feb 15;332:108537.
[4]Bosch AJ, Keller L, Steiger L, Rohm TV, Wiedemann SJ, Low AJ, Stawiski M, Rachid L, Roux J, Konrad D, Wueest S. CSF1R inhibition with PLX5622 affects multiple immune cell compartments and induces tissue-specific metabolic effects in lean mice. Diabetologia. 2023 Dec;66(12):2292-306.
| Cell experiment [1]: | |
|
Cell lines |
Primary mixed mouse astrocytes and microglia cells |
|
Preparation Method |
Primary mixed mouse astrocytes and microglia cells were extracted from newborn C57BL/6 mice[1]. Cells were divided into PLX5622 group and control group, and were incubated in DMEM media[1]. 10mg PLX5622 was dissolved in 1.25ml DMSO to prepare a 20mM of stock solution. Then the PLX5622 group was treated with 10μM, while control group only involved DMSO[1]. The media with either PLX5622 or DMSO was exchanges every three days[1]. At day 6, 12, 28, 42, cells were fixed for proliferation analysis[1]. |
|
Reaction Conditions |
PLX5622: 10μM; Day 6, 12, 28, 42 |
|
Applications |
10μM PLX5622 starting im-mediately after cell extraction reduced microglial cell number to 8% of the control group. And starting at day in vitro 12, cell number was reduced to 25% of the control group. After 4 weeks treatment, number of microglial decreased to 2%, then dropped to less than 0.5% after 6 weeks. The elimination of microglial was slow, where the half-time was 6 days. |
| Animal experiment [2]: | |
|
Animal models |
C57BL/6Nctrl mice |
|
Preparation Method |
PLX5622 group mice were fed a diet with PLX5622 at 1200mg/kg, while control group mice were fed a diet with AIN76 at a concentration of 1200mg/kg for 5 months[2]. PLX5622 group mice were injected 1mg/mouse anti-mouse CD115 antibody; control group mice were injected rat IgG2a isotype control by weekly for 3 weeks to estimate macrophage depletion[2]. A recovery assay was performed by 4 weeks PLX5622-supplemnt then 3-4 weeks control diet[2]. After euthanasia, immune cells were isolated to perform flow cytometry[2]. |
|
Dosage form |
PLX5622: 1200mg/kg; 5 months; AIN76: 1200mg/kg; 5 months |
|
Applications |
After 5 months diet, a 95% reduction of microglia was observed in PLX5622 group mice. Resident macrophages in multiple organs were depleted, including colon (92.4%); adipose tissue (58.2%); lung (26.3%) and peritoneal cavity (90.2%). However, a recovery of microglia has been observed after removal of PLX5622. The same repopulation was also shown in bone marrow and spleen, indicating that immune cells could revert after withdrawal of PLX5622. |
|
References: |
|
| Cas No. | 1303420-67-8 | SDF | |
| Canonical SMILES | COC1=NC=C(F)C=C1CNC2=NC(F)=C(CC3=CNC4=NC=C(C)C=C43)C=C2 | ||
| Formula | C21H19F2N5O | M.Wt | 395.41 |
| Solubility | DMSO: 83.33 mg/mL (210.74 mM); Water: < 0.1 mg/mL (insoluble) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.529 mL | 12.6451 mL | 25.2902 mL |
| 5 mM | 505.8 μL | 2.529 mL | 5.058 mL |
| 10 mM | 252.9 μL | 1.2645 mL | 2.529 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 2 reference(s) in Google Scholar.)