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编 号:F448023
分子式:C16H11Cl2FO2
分子量:325.16
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10mM*1mL in DMSO
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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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生物活性:
Itanapraced (CHF5074) is an orally active γ-secretase modulator and a non-steroidal anti-inflammatory derivative. Itanapraced reduces Aβ42 and Aβ40 secretion with IC50 values of 3.6 and 18.4 μM, respectively. Itanapraced inhibits cell apoptosis of hippocampal neurons induced by oxygen and glucose deprivation (OGD). Itanapraced can be used for the research of Alzheimer's disease.

体内研究:
Itanapraced (口服;375 ppm 加入饮食中,17 周) 在 Tg2576 转基因小鼠降低 Aβ42 和 Aβ40 水平以及脑斑块负担。Animal Model:Male and female Tg2576 transgenic mice expressing Swedish mutated form of human APP (APPswe)
Dosage:375 ppm
Administration:Oral administration; 375 ppm in the diet for 17 weeks
Result:Reduced total brain Aβ42 and Aβ40 levels, and brain plaque burden in aged Tg2576 mice. Caused no COX-mediated toxic effects in the gastrointestinal tract and Notch-mediated cell differentiation abnormalities in the ileum.

体外研究:
Itanapraced (0.03-100 μM) 抑制表达 APPswe 的人神经胶质瘤细胞 (H4swe) 分泌,对 Aβ42 和 Aβ40 的 IC50 值分别为 3.6 和 18.4 μM。Itanapraced (5-200 μM) 在浓度大于 15 μM 时,抑制 HEK293swe 细胞的 Notch 加工。Itanapraced (0-1000 μM; 30 min) 剂量依赖性抑制动作电位,IC50 值为 106 μM。Itanapraced (30-100 μM) 剂量依赖性地抑制兴奋性突触传递。Itanapraced (1-10 μM) 能显著降低缺氧葡萄糖 (OGD) 诱导的海马神经元细胞凋亡。
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