|Description||CHF5074, also known as CSP-1103, is a novel γ-secretase modulator. It could reduce Aβ42 and Aβ40 secretion, which IC50 value is 3.6 and 18.4 μM respectively. It induces microglia alternative activation in plaque-free Tg2576 mice and primary glial cultures exposed to beta-amyloid. It restores visual memory ability and pre-synaptic cortical acetylcholine release in pre-plaque Tg2576 mice. In vitro, it significantly reduces the area occupied by plaques and the number of plaques in cortex and hippocampus. It reduces brain beta-Amyloid pathology in a transgenic mouse model of Alzheimer's Disease without causing peripheral toxicity. It is a non-steroidal anti-inflammatory derivative holding disease-modifying potential for the treatment of Alzheimer's disease. It significantly reduces the apoptosis in hippocampal neurons exposed to OGD, as revealed by cleaved-caspase-3 immunoreactivity and TUNEL staining. It protects SH-SY5Y human neuronal-like cells from amyloidbeta 25-35 and tumor necrosis factor related apoptosis inducing ligand toxicity in vitro. In vivo, it was well tolerated by Tg2576 mice. It is orally well absorbed (50%), and it is slowly eliminated from plasma in rats.|
|Synonyms||CSP-1103;1-[4-(3,4-dichlorophenyl)-3-fluorophenyl]cyclopropane-1-carboxylic acid;1-(3′,4′-Dichloro-2-fluoro[1,1′-biphenyl]-4-yl)-cyclopropanecarboxylic acid|
|Application||CHF5074 induces microglia alternative activation in plaque-free Tg2576 mice and primary glial cultures exposed to beta-amyloid. It restores visual memory ability and pre-synaptic cortical acetylcholine release in pre-plaque Tg2576 mice. It is a non-steroidal anti-inflammatory derivative holding disease-modifying potential for the treatment of Alzheimer's disease. It significantly reduces the apoptosis in hippocampal neurons exposed to OGD, as revealed by cleaved-caspase-3 immunoreactivity and TUNEL staining.|
|Quality Standard||In-house standard|
|Shelf Life||2 month in rt, long time|
|Boiling Point||466.4±45.0 °C | Condition: Press: 760 Torr|
|Density||1.467±0.06 g/cm3 | Condition: Temp: 20 °C Press: 760 Torr|
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