CHF 5074 Property

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)

Safety

Hazard Codes 

Xn,N

Risk Statements 

22-50/53

Safety Statements 

60-61

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H320Causes eye irritation

H335May cause respiratory irritation

Precautionary statements

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P330Rinse mouth.

CHF 5074 Chemical Properties,Usage,Production

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