Name | CHF5074 |
Synonyms | CHF5074 CHF 5074 CSP-1103 GHF-5074 Itanapraced 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 |
CAS | 749269-83-8 |
Molecular Formula | C16H11Cl2FO2 |
Molar Mass | 325.16 |
Density | 1.467±0.06 g/cm3(Predicted) |
Boling Point | 466.4±45.0 °C(Predicted) |
Solubility | DMSO: ≥ 37 mg/mL |
pKa | 2.30±0.20(Predicted) |
Storage Condition | 2-8°C |
In vitro study | In glioma cells expressing APPswe (H4swe), CHF5074 reduced Aβ42 release with an IC50 of 3.6 μm. At concentrations up to 100 μm and 300 μm, CHF5074 had no inhibitory activity against COX-1 and COX-2. |
In vivo study | In rats, CHF5074 is well absorbed orally (50%) and slowly eliminated in plasma (half-life approximately 20 hours). In Tg2576 transgenic mice, long-term treatment with CHF5074 significantly reduced the total amount of Aβ in the brain, while no Notch-mediated toxicity was found at the histological level. |
Risk Codes | R22 - Harmful if swallowed R50/53 - Very toxic to aquatic organisms, may cause long-term adverse effects in the aquatic environment. |
Safety Description | S60 - This material and its container must be disposed of as hazardous waste. S61 - Avoid release to the environment. Refer to special instructions / safety data sheets. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 3.075 ml | 15.377 ml | 30.754 ml |
5 mM | 0.615 ml | 3.075 ml | 6.151 ml |
10 mM | 0.308 ml | 1.538 ml | 3.075 ml |
5 mM | 0.062 ml | 0.308 ml | 0.615 ml |
biological activity | Itanapraced (CHF 5074, CSP-1103) is a gamma-secretase modulator that reduces the secretion of Aβ42 and aβ40. It inhibits COX1 and COX2 with an IC50 greater than 100 μm. |
Target | Value |