产品说明书
PLX5622
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同义名 : | - |
| CAS号 : | 1303420-67-8 | |
| 货号 : | A1189464 | |
| 分子式 : | C21H19F2N5O | |
| 纯度 : | 99%+ | |
| 分子量 : | 395.405 | |
| MDL号 : | MFCD32201039 | |
| 存储条件： |
粉末 Keep in dark place,Sealed in dry,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 65 mg/mL(164.39 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO 无水乙醇: 3 mg/mL(7.59 mM)，配合低频超声，并水浴加热至45℃助溶，注意：无水乙醇开封后，易挥发，也会吸收空气中的水分，导致溶解能力下降，请避免使用开封较久的乙醇 |
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| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | icroglia are the resident immune cells in the central nervous system. The Colony-stimulating factor-1 receptor (CSF-1R) is expressed by microglia, macrophages and osteoclasts, and is required for their proliferation, differentiation, and survival. PLX5622 is an orally bioavailable, brain-penetrant and highly selective CSF-1R inhibitor with IC50 < 10 nM, showing > 20-fold selectivity over KIT and FLT3[1]. Oral PLX5622 (1200 ppM) treatment in 5xFAD mice model of Alzheimer’s disease with increased numbers of microglia/myeloid cells and masses of enlarged, plaque-associated cells throughout the brain led to almost complete microglial elimination (97–100% reduction), even with 24 weeks of treatment[1]. Approximately 99% of microglia were eliminated by embryonic day 15.5 (E15.5) and numbers of apoptotic cells accumulating throughout the developing hypothalamus were elevated after pregnant dams were placed on a PLX5622 diet starting at E3.5[2]. | ||
| 作用机制 | PLX5622 is anchored to the active site of CSF1R by 3 hydrogen bonds. 7-Azaindole of PLX5622 forms two hydrogen bonds with the hinge region of CSF1R whereas the central pyridine ring forms a hydrogen bond with the main chain amino group of Phe796. | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.53mL 0.51mL 0.25mL |
12.65mL 2.53mL 1.26mL |
25.29mL 5.06mL 2.53mL |
| 参考文献 |
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