产品
编 号：F044855
分子式：C27H35N5O2
分子量：461.6
分子式：C27H35N5O2
分子量：461.6
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
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1mg
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5mg
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10mg
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25mg
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50mg
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100mg
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结构图
CAS No: 1142363-52-7
产品详情
生物活性：
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. Edicotinib limits microglial expansion and attenuates microglial proliferation and neurodegeneration?in mice. Edicotinib has the potential for Alzheimer’s disease and rheumatoid arthritis research.
体内研究：
Edicotinib (oral gavage; 3, 10, 30 and 100 mg/kg; 5 days) 显著抑制 ME7 小鼠的小胶质细胞增殖。 Edicotinib 具有良好的药代动力学/药效学 (PK/PD) 特征。 Edicotinib (口服灌胃；30 mg/kg；33天) 显著降低 ME7-prion 小鼠海马 CA1 区小胶质细胞密度 (PU.1+ 细胞) 高达 30%。IL-1β的表达也降低，但其他炎性细胞因子不受影响。Animal Model:C57BL/6 J (Harlan) mice?
Dosage:3, 10, 30 and 100 mg/kg; 5 days
Administration:Oral gavage
Result:Did not affect microglial numbers when administered under 100 mg/kg.
Animal Model:C57BL/6 J (Harlan) mice?
Dosage:30 mg/kg; 33 days
Administration:Oral gavage
Result:Limited microglial expansion and attenuated behavioural deficits in ME7-prion mice.
体外研究：
Edicotinib (0.1 nM-1 μM；24 小时) 导致 CSF1R 激活剂量依赖性降低，并同时降低 ERK1 和 ERK2 磷酸化。剂量反应曲线显示 JNJ-527 对 CSF1R 和 ERK1/2 的影响，对 CSF1R 和 ERK1/2 的 IC50 值分别为 18.6 nM 和 22.5 nM。
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. Edicotinib limits microglial expansion and attenuates microglial proliferation and neurodegeneration?in mice. Edicotinib has the potential for Alzheimer’s disease and rheumatoid arthritis research.
体内研究：
Edicotinib (oral gavage; 3, 10, 30 and 100 mg/kg; 5 days) 显著抑制 ME7 小鼠的小胶质细胞增殖。 Edicotinib 具有良好的药代动力学/药效学 (PK/PD) 特征。 Edicotinib (口服灌胃；30 mg/kg；33天) 显著降低 ME7-prion 小鼠海马 CA1 区小胶质细胞密度 (PU.1+ 细胞) 高达 30%。IL-1β的表达也降低，但其他炎性细胞因子不受影响。Animal Model:C57BL/6 J (Harlan) mice?
Dosage:3, 10, 30 and 100 mg/kg; 5 days
Administration:Oral gavage
Result:Did not affect microglial numbers when administered under 100 mg/kg.
Animal Model:C57BL/6 J (Harlan) mice?
Dosage:30 mg/kg; 33 days
Administration:Oral gavage
Result:Limited microglial expansion and attenuated behavioural deficits in ME7-prion mice.
体外研究：
Edicotinib (0.1 nM-1 μM；24 小时) 导致 CSF1R 激活剂量依赖性降低，并同时降低 ERK1 和 ERK2 磷酸化。剂量反应曲线显示 JNJ-527 对 CSF1R 和 ERK1/2 的影响，对 CSF1R 和 ERK1/2 的 IC50 值分别为 18.6 nM 和 22.5 nM。
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