DIBENZAZEPINE
Synonym(s):DBZ;Dibenzazepine;GSI-XX;N-[(1S)-2-[[(7S)-6,7-Dihydro-5-methyl-6-oxo-5H-dibenz[b,d]azepin-7-yl]amino]-1-methyl-2-oxoethyl]-3,5-difluoro-benzeneacetamide;γ-Secretase inhibitor XX
- CAS NO.:209984-56-5
- Empirical Formula: C26H23F2N3O3
- Molecular Weight: 463.48
- MDL number: MFCD12828734
- SAFETY DATA SHEET (SDS)
- Update Date: 2023-06-30 15:45:59
What is DIBENZAZEPINE?
Description
γ-
Chemical properties
White Solid
The Uses of DIBENZAZEPINE
DIBENZAZEPINE is a dipeptidic-secretase inhibitor and a antiAlzheimer agent.
The Uses of DIBENZAZEPINE
A dipeptidic γ-secretase inhibitor. AntiAlzheimer agent.
The Uses of DIBENZAZEPINE
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%.
What are the applications of Application
Dibenzazepine (Deshydroxy LY 411575) is a dipeptidic (c)-secretase inhibitor
General Description
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 ApcMin mouse models (10 μmol/kg, i.p).
Biochem/physiol Actions
Cell permeable: yes
storage
-20°C
Properties of DIBENZAZEPINE
Melting point: | 257-259?C |
Boiling point: | 801.3±65.0 °C(Predicted) |
Density | 1.35 |
storage temp. | -20°C |
solubility | DMSO: soluble15mg/mL, clear |
pka | 12.76±0.20(Predicted) |
form | White solid |
color | white to beige |
Safety information for DIBENZAZEPINE
Computed Descriptors for DIBENZAZEPINE
InChIKey | QSHGISMANBKLQL-OWJWWREXSA-N |
New Products
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