PLX5622-hemifumarate-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEPLX5622 hemifumarateCat. No.: HY-114153A分式: CHFNO分量: 453.45作靶点: c-Fms作通路: Protein Tyrosine Kinase/RTK储存式: 4C, stored under nitrogen* In solvent : -80C, 6 months; -20C, 1 month (stored undernitrogen)溶解性数据体外实验 DMSO : 100 mg/mL (22

2、0.53 mM; Need ultrasonic)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (5.51 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (5.51 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (5.51 mM); Clear solution1/2 Master

3、of Small Molecules 您边的抑制剂师www.MedChemEBIOLOGICAL ACTIVITY物活性 PLX5622 hemifumarate度选择性的、能透过脑屏障的、服有效的 CSF1R 抑制剂，Ki 值为 5.9 nM，可于病程发展前和过程中，扩的和特异性的胶质细胞的消除。PLX5622 hemifumarate 具有较好的药理学特性。IC50 & Target CSF1R 1体内研究 PLX5622 hemifumarate (oral gavage; 65 mg/kg/day; for 14 days) causes paw withdrawal threshol

4、d high inmice, 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) 2Dosage: 65 mg/kgAdministration: Oral gavage; daily; for 14 daysResult: Caused paw withdrawal threshold high in mice, and prevented

5、 the development of injury-associated mechanical allodynia.REFERENCES1. Spangenberg E, et al. Sustained microglial depletion with CSF1R inhibitor impairs parenchymal plaque development in an Alzheimersdisease 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 totreat injury-triggered neuropathic pain. Mol Pain. 2018 Jan-Dec;14:1744806918764979.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use only.Tel: 400-820-