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  • Edicotinib

    • JNJ-40346527;JNJ-527
    货号: abs820234
    CAS号: 1142363-52-7
    分子式: C27H35N5O2
    分子量: 461.60
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    货号-规格 货期 价格 数量
    abs820234-5mg 1-2周 ¥1850.00
    - +
    abs820234-25mg 1-2周 ¥6550.00
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    大包装询价
    产品描述
    描述
    Edicotinib (JNJ-40346527) is a potent, selective, brain penetrant and orally active colony-stimulating factor-1 receptor (CSF-1R) inhibitor with an IC50 of 3.2 nM. Edicotinib exhibits less inhibitory effects on KIT and FLT3 with IC50 values of 20 nM and 190 nM, respectively[1]. Edicotinib limits microglial expansion and attenuates microglial proliferation and neurodegeneration in mice. Edicotinib has the potential for Alzheimer’s disease and rheumatoid arthritis research.
    纯度
    98%
    储存/保存方法
    Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
    基本信息
    别名
    JNJ-40346527;JNJ-527
    可溶性/溶解性
    DMSO : 16.67 mg/mL (36.11 mM; Need ultrasonic)
    生物活性
    靶点
    CSF-1 receptor
    In vitro(体外研究)
    Edicotinib (0.1 nM-1μM; 24 hours) Leads to a dose-dependent decrease of CSF1R activation and a concurrent reduction of ERK1 and ERK2 phosphorylation. The dose response curve shows the effect of JNJ-527 on CSF1R and ERK1/2, and the IC50 values are 18.6 nM and 22.5 nM for CSF1R and ERK1/2, respectively.
    In vivo(体内研究)
    Edicotinib (oral gavage; 3, 10, 30 and 100 mg/kg; 5 days) significantly inhibits microglial proliferation in ME7 mice. It diminishes the number of microglia (total CD45+CD11b+ cells) only at the highest dose tested of 100 mg/kg, and JNJ-527 depletes up to 50% of patrolling blood monocytes at every dose tested (CD45+CD11bhighLy6Cintermediate/lowcells) with only a tendency for a reduction in the proportion of inflammatory monocytes (Ly6C high cells) at 100 mg/kg.
    Edicotinib exhibits a good pharmacokinetic/pharmacodynamics (PK/PD) profile, the microglial proliferation data shows an EC50 of 196/ml and 69 ng/g calculated from plasmatic and brain compound concentration, respectively.
    Edicotinib (oral gavage; 30 mg/kg; 33 days) significantly reduces the density of microglia in CA1 of the hippocampus of ME7-prion mice (PU.1+ cells) by up to 30%. And the expression of IL-1β is also reduced,but not other inflammatory cytokines.
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    • 实验方法 实验条件
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