209984-56-5 Usage
Description
DIBENZAZEPINE, also known as DBZ, is a cell-permeable, potent γ-secretase inhibitor that significantly lowers both brain and plasma Aβ40 levels. It is a dipeptidic compound with a white solid appearance, playing a crucial role in the treatment of Alzheimer's disease by inhibiting the proteolysis of amyloid precursor protein (APP) and other type 1 transmembrane proteins.
Uses
Used in Pharmaceutical Industry:
DIBENZAZEPINE is used as an anti-Alzheimer agent for its ability to reduce Aβ40 levels by 71% within 4 hours after a single 100 μM/kg dose in an APP transgenic mouse model. It 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), thus demonstrating its effectiveness in treating Alzheimer's disease.
Used in Research and Development:
DIBENZAZEPINE is used as a dipeptidic γ-secretase inhibitor in research and development for its potential to inhibit Notch processing and induce conversion of proliferative crypt cells to post-mitotic goblet cells in mouse models. This application aids in understanding the compound's effects on cellular processes and its potential therapeutic applications.
Biochem/physiol Actions
Cell permeable: yes
Check Digit Verification of cas no
The CAS Registry Mumber 209984-56-5 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 2,0,9,9,8 and 4 respectively; the second part has 2 digits, 5 and 6 respectively.
Calculate Digit Verification of CAS Registry Number 209984-56:
(8*2)+(7*0)+(6*9)+(5*9)+(4*8)+(3*4)+(2*5)+(1*6)=175
175 % 10 = 5
So 209984-56-5 is a valid CAS Registry Number.
InChI:InChI=1/C26H23F2N3O3/c1-15(29-23(32)13-16-11-17(27)14-18(28)12-16)25(33)30-24-21-9-4-3-7-19(21)20-8-5-6-10-22(20)31(2)26(24)34/h3-12,14-15,24H,13H2,1-2H3,(H,29,32)(H,30,33)/t15-,24-/m0/s1
209984-56-5Relevant articles and documents
CYCLOALKYL, LACTAM, LACTONE AND RELATED COMPOUNDS, PHARMACEUTICAL COMPOSITIONS COMPRISING SAME, AND METHODS FOR INHIBITING BETA-AMYLOID PEPTIDE RELEASE AND/OR ITS SYNTHESIS BY USE OF SUCH COMPOUNDS
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Page/Page column 62; 79, (2009/02/10)
Disclosed are compounds which inhibit beta -amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits beta -amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.