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| | DIBENZAZEPINE Basic information |
| | DIBENZAZEPINE Chemical Properties |
| 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 | | InChIKey | QSHGISMANBKLQL-OWJWWREXSA-N |
| Hazard Codes | Xi | | Risk Statements | 36/37/38 | | Safety Statements | 26 | | WGK Germany | 3 | | HS Code | 29337900 |
| | DIBENZAZEPINE Usage And Synthesis |
| 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. 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%. | | Chemical Properties | White Solid | | 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%. | | Uses | A dipeptidic γ-secretase inhibitor. AntiAlzheimer agent. | | 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 | -20°C |
| | DIBENZAZEPINE Preparation Products And Raw materials |
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