| Identification | Back Directory | [Name]
DIBENZAZEPINE | [CAS]
209984-56-5 | [Synonyms]
GSI-XX
CS-366
YO01027
DIBENZAZEPINE
Deshydroxy LY-411575
YO-01027 (Dibenzazepine)
Dibenzazepine (YO-01027)
γ-Secretase Inhibitor XX
γ-Secretase Inhibitor DBZ
DBZ, γ-Secretase Inhibitor
gamma-Secretase Inhibitor XX
YO-01027 (Dibenzazepine, DBZ)
YO-01027/Dibenzazepine/LY 411575
Dibenzazepine (Deshydroxy LY 411575)
Dibenzazepine (deshydroxy LY 411575) DBZ
Dibenzazepine, 98%, γ-secretase inhibitor
γ-Secretase Inhibitor XX - CAS 209984-56-5 - Calbiochem
YO-01027; YO01027; DIBENZAZEPINE; DESHYDROXY LY 411575;DBZ
(S)-2-(2-(3,5-Difluorophenyl)acetamido)-N-((S)-5-methyl-6-oxo-6,7-dihydro-5H-dibenzo[b,d]azepi
(S)-2-(2-(3,5-Difluorophenyl)acetamido)-N-((S)-5-methyl-6-oxo-6,7-dihydro-5H-dibenzo[b,d]azepin-7
(2S)-2-[2-(3,5-Difluorophenyl)acetaMide]-N-[(7S)-5-Methyl-6-oxo-6,7-dihydro-5H-dibenzo[B,D]azepin-7-
7-(S)-[N'(3,5-difluorophenylacetyl)-L-alaninyl]amino-5-methyl-5,7-dihydro-6H-dibenz[b,d]azepin-6-one
(S,S)-2-[2-(3,5-Difluorophenyl)acetylamino]-N-(5-methyl-6-oxo-6,7-dihydro-5H-dibenzo[b,d]azepin-7-yl)propionamide
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-difluorobenzeneacetamide
Benzeneacetamide, 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- | [Molecular Formula]
C26H23F2N3O3 | [MDL Number]
MFCD12828734 | [MOL File]
209984-56-5.mol | [Molecular Weight]
463.48 |
| Chemical Properties | Back Directory | [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 | [form ]
White solid | [pka]
12.76±0.20(Predicted) | [color ]
white to beige | [optical activity]
[α]/D -128.0 to -154.0°-0.25 in methanol | [InChIKey]
QSHGISMANBKLQL-OWJWWREXSA-N |
| Hazard Information | Back Directory | [Description]
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 ErbB4.1 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.2 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).3 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%.3 | [Chemical Properties]
White Solid | [Uses]
A dipeptidic γ-secretase inhibitor. AntiAlzheimer agent. | [Uses]
DIBENZAZEPINE is a dipeptidic-secretase inhibitor and a antiAlzheimer agent.
| [Uses]
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%. | [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 | [target]
APPL | [storage]
Store at -20°C |
|
|