| Identification | Back Directory | [Name]
CHF 5074 | [CAS]
749269-83-8 | [Synonyms]
CHF 5074
GHF-5074
CSP-1103
Itanapraced
1-[4-(3,4-dichlorophenyl)-3-fluorophenyl]cyclopropane-1-carboxylic Acid
1-(3′,4′-Dichloro-2-fluoro[1,1′-biphenyl]-4-yl)-cyclopropanecarboxylic acid
Cyclopropanecarboxylic acid, 1-(3',4'-dichloro-2-fluoro[1,1'-biphenyl]-4-yl)-
1-[4-(3,4-dichlorophenyl)-3-fluorophenyl]cyclopropane-1-carboxylic acid GHF-5074 | [Molecular Formula]
C16H11Cl2FO2 | [MDL Number]
MFCD18633206 | [MOL File]
749269-83-8.mol | [Molecular Weight]
325.16 |
| Chemical Properties | Back Directory | [Boiling point ]
466.4±45.0 °C(Predicted) | [density ]
1.467±0.06 g/cm3(Predicted) | [storage temp. ]
2-8°C | [solubility ]
DMSO:59.0(Max Conc. mg/mL);181.45(Max Conc. mM) | [form ]
A solid | [pka]
2.30±0.20(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Biological Activity]
Itanapraced (CHF 5074, CSP-1103) is a gamma-secretase modulator that reduces Aβ42 and Aβ40 secretion. It inhibits COX1 and COX2 with IC50 greater than 100 μM. | [in vitro]
In glioma cells expressing APPswe (H4swe), CHF5074 reduces Aβ42 release with IC50 of 3.6 μM. It had no inhibitory activity against COX-1 and COX-2 at concentrations up to 100 μM and 300 μM. | [in vivo]
In rats, CHF5074 is well absorbed orally (50%) and is slowly eliminated from plasma (half-life approximately 20 hours). In Tg2576 transgenic mice, chronic treatment of CHF5074 significantly reduced the total amount of Aβ in the brain, and at the histological level, no Notch-mediated toxic effects were found. | [target]
| Target | Value | γ secretase
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Tags:749269-83-8
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