PLX5622
目录号 : GC36940
PLX5622是一种集落刺激因子1受体（CSFR1）的选择性抑制剂，IC50值为0.016μM。
Cas No.:1303420-67-8
Sample solution is provided at 25 µL, 10mM.
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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.
PLX5622是一种集落刺激因子1受体（CSFR1）的选择性抑制剂，IC50值为0.016μM[1]。PLX5662主要作用于中枢神经系统中的小胶质细胞[2]。通过抑制 CSFR1受体，PLX5662 选择性地清除小胶质细胞，而不影响其他类型的骨髓细胞[2]。PLX5662是研究小胶质细胞在神经退行性疾病中作用的工具[2]。
在体外，提取原代混合小鼠星形胶质细胞和小胶质细胞[3]。细胞用10 μM PLX5622（用20 mM DMSO母液液稀释）处理，其他对照细胞仅用DMSO处理[3]。用10 μM PLX5622处理小胶质细胞后，从细胞提取后立即开始的细胞数量减少到对照组的8%，而从体外培养第12天开始的细胞数量则只减少到对照组的25%[3]。4 周后，小胶质细胞数量下降至 2%，6周后下降至不足0.5%[3]。PLX5622显著抑制了小胶质细胞的生长。
在体内，C57BL/6NCrl小鼠饲喂剂量1200mg/kg的PLX5622饮食，而对照组饲喂相同浓度的AIN76饮食[4]。5个月后，观察到小鼠的小胶质细胞减少了95%[4]。多个器官中的常驻巨噬细胞被耗尽，包括结肠（92.4%）；脂肪组织（58.2%）；肺（26.3%）和腹膜腔（90.2%）[4]。然而，在去除PLX5622后观察到小胶质细胞的恢复[4]。骨髓和脾脏中也显示出相同的重新增殖，表明免疫细胞在停止PLX5622后可以恢复[4]。
| 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 | ||
| 分子式 | C21H19F2N5O | 分子量 | 395.41 |
| 溶解度 | DMSO: 83.33 mg/mL (210.74 mM); Water: < 0.1 mg/mL (insoluble) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.529 mL | 12.6451 mL | 25.2902 mL |
| 5 mM | 0.5058 mL | 2.529 mL | 5.058 mL |
| 10 mM | 0.2529 mL | 1.2645 mL | 2.529 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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