DIBENZAZEPINE

Bezeichnung:DIBENZAZEPINE

CAS-Nr209984-56-5

Englisch Name:DIBENZAZEPINE

CBNumberCB11234300

SummenformelC26H23F2N3O3

Molgewicht463.48

MOL-Datei209984-56-5.mol

DIBENZAZEPINE physikalisch-chemischer Eigenschaften

Schmelzpunkt	257-259?C
Siedepunkt	801.3±65.0 °C(Predicted)
Dichte	1.35
storage temp.	-20°C
Löslichkeit	DMSO: soluble15mg/mL, clear
Aggregatzustand	White solid
pka	12.76±0.20(Predicted)
Farbe	white to beige
InChIKey	QSHGISMANBKLQL-OWJWWREXSA-N

Sicherheit

Kennzeichnung gefährlicher	Xi
R-Sätze:	36/37/38
S-Sätze:	26
WGK Germany	3
HS Code	29337900

Gefahreninformationscode (GHS)

DIBENZAZEPINE Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
γ-Secretase is a multi-subunit aspartyl protease that cleaves amyloid precursor protein (APP) and many other type 1 transmembrane proteins, including Notch, E-cadherin, and ErbB4. The proteolysis of APP by secretases produces beta amyloid (Aβ), a 39- to 42-amino acid peptide which forms the amyloid plaques that are characteristic of Alzheimer’s disease. DBZ is a dipeptidic inhibitor of γ-secretase that potently blocks the cleavage of Notch into its active signaling effector, Notch intracellular domain, in human T cell lymphoma (SupT1) cells (IC₅₀ = 1.7 nM). Within 4 hours after a single 100 μM/kg dose, DBZ demonstrates anti-Alzheimer activity in an APP transgenic mouse model characterized by high levels of Aβ40 by reducing Aβ40 levels by 71%.
Chemische Eigenschaften
White Solid
Verwenden
γ-Secretase is a multi-subunit aspartyl protease that cleaves amyloid precursor protein (APP) and many other type 1 transmembrane proteins, including Notch, E-cadherin, and ErbB4. The proteolysis of APP by secretases produces beta amyloid (Aβ), a 39- to 42-amino acid peptide which forms the amyloid plaques that are characteristic of Alzheimer’s disease. DBZ is a dipeptidic inhibitor of γ-secretase that potently blocks the cleavage of Notch into its active signaling effector, Notch intracellular domain, in human T cell lymphoma (SupT1) cells (IC50 = 1.7 nM). Within 4 hours after a single 100 μM/kg dose, DBZ demonstrates anti-Alzheimer activity in an APP transgenic mouse model characterized by high levels of Aβ40 by reducing Aβ40 levels by 71%.
Verwenden
DIBENZAZEPINE is a dipeptidic-secretase inhibitor and a antiAlzheimer agent.
Verwenden
A dipeptidic γ-secretase inhibitor. AntiAlzheimer agent.
Allgemeine Beschreibung
A cell-permeable, potent γ-secretase inhibitor that significantly lowers both brain and plasma Aβ₄₀ levels by ~72% in Tg2576 mutant APP transgenic mouse model (100 μmol/kg, b.i.d). Induces a heterogeneous reorganization of the crypt structural-proliferative units in the intestinal tract and of the stem cell niche in the colon. Also potently inhibits Notch processing (IC₅₀ = 1.7 nM in SupT1 cells) and induces conversion of proliferative crypt cells to post-mitotic goblet cells in both the C57BL/6 and Apc^Min mouse models (10 μmol/kg, i.p).
Biochem/physiol Actions
Cell permeable: yes
target
APPL
Lager
-20°C

DIBENZAZEPINE Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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