Bioactivity | 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[1][2]. | ||||||||||||
Invitro | 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[1]。Itanapraced (5-200 μM) 在浓度大于 15 μM 时,抑制 HEK293swe 细胞的 Notch 加工[1]。Itanapraced (0-1000 μM; 30 min) 剂量依赖性抑制动作电位,IC50 值为 106 μM[2]。Itanapraced (30-100 μM) 剂量依赖性地抑制兴奋性突触传递[2]。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[2]。 | ||||||||||||
Name | Itanapraced | ||||||||||||
CAS | 749269-83-8 | ||||||||||||
Formula | C16H11Cl2FO2 | ||||||||||||
Molar Mass | 325.16 | ||||||||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
Storage |
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