PLX5622 是高度选择性的、能透过血脑屏障的、口服有效的 CSF1R 抑制剂,可用于病程发展前和过程中,扩大的和特异性的小胶质细胞的消除。 PLX5622 具有较好的药理学特性。 Information PLX5622 PLX5622 is a highly selective CSF-1R inhibitor (IC50 20-fold selectivity over KIT and FLT3. Targets CSF-1R (Cell-free assay); FLT3 (Cell-free assay); KIT (Cell-free assay); AURKC (Cell-free assay); KDR (Cell-free assay) ;0.016 μM; 0.39 μM; 0.86 μM; 1 μM; 1.1 μM In vivo In vivo PLX5622 demonstrates desirable PK properties in mice, rats, dogs, and monkeys, with a brain penetrance of ~20%. PLX5622 has low systemic clearance, moderate volume of distribution, and favorable oral bioavailability (F > 30%) in all four species. PLX5622 is a useful compound for investigating microglial dynamics. It allows for the sustained and specific elimination of microglia, preceding and during pathology development of Alzheimer’s disease (AD). Long-term PLX5622-mediated microglial depletion is highly robust, sustainable, and specific to the microglial compartment.
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PLX5622
Dangerous GoodsCAS number:1303420-67-8 molecular formula:C21H19F2N5O
overview
compound introduction
Specs
| Chinese alias | - | ||
| English alias | 3-Pyridinemethanamine, 5-fluoro-N-(6-fluoro-5-((5-methyl-1H-pyrrolo(2,3-b)pyridin-3-yl)methyl)-2-pyridinyl)-2-methoxy- | HY-114153 | 6-Fluoro-N-((5-fluoro-2-methoxypyridin-3-yl)methyl)-5-((5-methyl-1H-pyrrolo[2,3-b]pyridin-3-yl)methyl)pyridin-2-amine | ZB | ||
| CAS number | 1303420-67-8 | molecular formula | C21H19F2N5O |
| molecular weight | 395.41 g/mol | Exact mass | - |
| PSA | 75.700 Ų | logp | 4.577 |
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physicochemical properties
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Safety information
pictogram:
GHS07
Signal word:
Warning
Hazard Statement:
H315: 引起皮肤刺激 H319: 引起严重眼睛刺激 H335: 可能引起呼吸道刺激 H302: 吞食有害
Statement of Preventive Measures:
P261: 避免吸入灰尘/烟雾/气体/雾/蒸汽/喷雾 P305+P351+P338: 如进入眼睛:用水小心冲洗几分钟。如戴隐形眼镜并可方便地取出,取出隐形眼镜。继续冲洗。 P280: 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。 P302+P352: 如皮肤沾染:用水充分清洗。 P301+P312: 如误吞咽:如感觉不适,呼叫急救中心/医生。
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