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ChemicalBook--->CAS DataBase List--->749269-83-8

749269-83-8

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      • 749269-83-8 Structure

        749269-83-8 Structure
        IdentificationBack 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 PropertiesBack 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
        Safety DataBack Directory
        [Hazard Codes ]

        Xn,N
        [Risk Statements ]

        22-50/53
        [Safety Statements ]

        60-61
        Hazard InformationBack 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]

        < /table>
        TargetValue
        γ secretase
        ()
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