CHF 5074

Product NameCHF 5074
CAS749269-83-8
MFC16H11Cl2FO2
MW325.16
EINECS
MOL File749269-83-8.mol

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)
color	White to off-white

Safety Information

Hazard Codes	Xn,N
Risk Statements	22-50/53
Safety Statements	60-61

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

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Target	Value
γ secretase ()