"目录号: HY-14399
Neuronal SignalingStem Cell/Wnt-
CHF5074是一种新型γ-secretase调节剂, 降低 Aβ42 和Aβ40 分泌, IC50分别为3.6和18.4 μM。
相关产品
DAPT-RO4929097-LY-411575-PF-3084014-BMS-708163-L-685458-Semagacestat-MK-0752-YO-01027-E 2012-gamma-secretase modulator 3-gamma-secretase modulator 1-Z-Ile-Leu-aldehyde-BMS 299897-BMS 433796-
生物活性
Description
CHF5074 is a novel γ-secretase modulator, reduces Aβ42 and Aβ40 secretion, with an IC50 of 3.6 and 18.4 μM, respectively.IC50 value: 3.6 μM (Aβ42), 18.4 μM (Aβ40) [1]Target: γ-secretasein vitro: CHF5074 significantly reduces the area occupied by plaques and the number of plaques in cortex and hippocampus. CHF5074 concentration reach in the brain (6.4 μM) were enough to efficiently inhibit A42 secretion (cell-based IC50 3.6 μM). CHF5074 reduces brain beta-Amyloid pathology in a transgenic mouse model of Alzheimer's Disease without causing peripheral toxicity. [1] CHF5074 is a non-steroidal anti-inflammatory derivative holding disease-modifying potential for the treatment of Alzheimer's disease. CHF5074 significantly reduces the apoptosis in hippocampal neurons exposed to OGD, as revealed by cleaved-caspase-3 immunoreactivity and TUNEL staining.[2]in vivo: CHF5074 was well tolerated by Tg2576 mice. In rats, CHF5074 is orally well absorbed (50%), and it is slowly eliminated from plasma. In young Tg2576 transgenic mice, short-term oraldosing with CHF5074 causes dose-dependent reduction ofplasma Aβ42. [1]
Clinical Trial
CERESPIR
Alzheimer's Disease
September 2010
Phase 1
CERESPIR
Alzheimer's Disease
September 2010
Phase 1
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