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PLX5622 hemifumarate
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
PLX5622 hemifumarate图片
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
1mg电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品介绍
PLX5622 hemifumarate 是高度选择性的、能透过血脑屏障的、口服有效的 CSF1R 抑制剂,Ki 值为 5.9 nM,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 hemifumarate 具有较好的药理学特性。
Canonical SMILESCOC1=NC=C(F)C=C1CNC2=NC(F)=C(CC3=CNC4=NC=C(C)C=C43)C=C2.O=C(O)/C=C/C(O)=O.[1/2]
分子式C23H21F2N5O3
分子量453.45
溶解度DMSO: 100 mg/mL (220.53 mM); Water:< 0.1 mg/mL (insoluble)
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

PLX5622 hemifumarate is a highly selective brain penetrant and oral active CSF1R inhibitor with an Ki of 5.9 nM, for extended and specific microglial elimination, preceding and during pathology development. PLX5622 hemifumarate demonstrates desirable PK properties in varies animals[1][2].

PLX5622 hemifumarate (oral gavage; 65 mg/kg/day; for 14 days) causes paw withdrawal threshold high in mice, indicating that PLX5622 prevents the development of injury-associated mechanical allodynia[2]. Animal Model: C57BL/6 mice (males, 10-12 weeks old, 20-25 g)[2]

[1]. Spangenberg E, et al. Sustained microglial depletion with CSF1R inhibitor impairs parenchymal plaque development in an Alzheimer's disease model. Nat Commun. 2019 Aug 21;10(1):3758. [2]. Lee S, et al. Targeting macrophage and microglia activation with colony stimulating factor 1 receptor inhibitor is an effective strategy to treat injury-triggered neuropathic pain. Mol Pain. 2018 Jan-Dec;14:1744806918764979.