CHF 5074 - CAS 749269-83-8
Catalog number: 749269-83-8
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C16H11Cl2FO2
Molecular Weight:
325.16
COA:
Inquire
Targets:
γ-secretase
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.
Purity:
98%
Appearance:
Solid powder
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
Solubility:
DMSO:37mg/mL
Storage:
-20°C Freezer
MSDS:
Inquire
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
Quantity:
Milligrams-Grams
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
InChIKey:
LIYLTQQDABRNRX-UHFFFAOYSA-N
InChI:
InChI=1S/C16H11Cl2FO2/c17-12-4-1-9(7-13(12)18)11-3-2-10(8-14(11)19)16(5-6-16)15(20)21/h1-4,7-8H,5-6H2,(H,20,21)
Canonical SMILES:
C1CC1(C2=CC(=C(C=C2)C3=CC(=C(C=C3)Cl)Cl)F)C(=O)O
1.CHF5074, a novel gamma-secretase modulator, attenuates brain beta-amyloid pathology and learning deficit in a mouse model of Alzheimer's disease.
Imbimbo BP;Hutter-Paier B;Villetti G;Facchinetti F;Cenacchi V;Volta R;Lanzillotta A;Pizzi M;Windisch M Br J Pharmacol. 2009 Mar;156(6):982-93. doi: 10.1111/j.1476-5381.2008.00097.x.
BACKGROUND AND PURPOSE: ;We evaluated the effects of 1-(3',4'-dichloro-2-fluoro[1,1'-biphenyl]-4-yl)-cyclopropanecarboxylic acid (CHF5074), a new gamma-secretase modulator, on brain beta-amyloid pathology and spatial memory in transgenic mice expressing the Swedish and London mutations of human amyloid precursor protein (hAPP).;EXPERIMENTAL APPROACH: ;Sixty 6-month-old hAPP mice were treated for 6 months with CHF5074 or ibuprofen (375 ppm in the diet) or standard diet. Twenty-one wild-type mice received standard diet.;KEY RESULTS: ;Compared with transgenic controls, CHF5074 treatment significantly reduced the area occupied by plaques in cortex (P = 0.003) and hippocampus (P = 0.004). The number of plaques were also reduced by CHF5074 in both cortex (P = 0.022) and hippocampus (P = 0.005). Plaque-associated microglia in CHF5074-treated animals was lower than in transgenic controls in cortex (P = 0.008) and hippocampus (P = 0.002). Ibuprofen treatment significantly reduced microglia area in cortex and hippocampus but not beta-amyloid burden. On the last day of the Morris water maze, transgenic controls performed significantly worse than the non-transgenic animals and the CHF5074-treated transgenic mice, on the swimming path to reach the hidden platform.
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