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| | CHF 5074 Basic information |
| Product Name: | CHF 5074 | | Synonyms: | CHF 5074;GHF-5074;1-[4-(3,4-dichlorophenyl)-3-fluorophenyl]cyclopropane-1-carboxylic acid GHF-5074;1-(3′,4′-Dichloro-2-fluoro[1,1′-biphenyl]-4-yl)-cyclopropanecarboxylic acid;1-[4-(3,4-dichlorophenyl)-3-fluorophenyl]cyclopropane-1-carboxylic Acid;Itanapraced;CSP-1103;Cyclopropanecarboxylic acid, 1-(3',4'-dichloro-2-fluoro[1,1'-biphenyl]-4-yl)- | | CAS: | 749269-83-8 | | MF: | C16H11Cl2FO2 | | MW: | 325.16 | | EINECS: | | | Product Categories: | Inhibitors | | Mol File: | 749269-83-8.mol |  |
| | CHF 5074 Chemical Properties |
| 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) |
| | CHF 5074 Usage And Synthesis |
| 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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| | CHF 5074 Preparation Products And Raw materials |
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Tag:CHF 5074(749269-83-8)
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