CHF 5074 Struktur

CHF 5074

Bezeichnung:CHF 5074

Englisch Name:CHF 5074

CBNumberCB62627687

SummenformelC16H11Cl2FO2

Molgewicht325.16

CHF 5074 physikalisch-chemischer Eigenschaften

Sicherheit

Kennzeichnung gefährlicher	Xn,N
R-Sätze:	22-50/53
S-Sätze:	60-61

Gefahreninformationscode (GHS)

Biologische Aktivität
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 ()