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A0455956

PhosphateBufferedSaline:1Lof10X

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.:

Empirical Formula: C26H23F2N3O3

Molecular Weight: 463.48

MDL number: MFCD12828734

Pack Size Price Stock Quantity
1L RMB195.20 In Stock
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Update time: 2022-07-08

PRODUCT 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

Description and 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%.

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%.

Safety

Symbol(GHS) 
GHS07
Signal word  Warning
Hazard statements  H335-H315-H319
Precautionary statements  P264-P280-P305+P351+P338-P337+P313P-P264-P280-P302+P352-P321-P332+P313-P362
Hazard Codes  Xi
Risk Statements  36/37/38
Safety Statements  26
WGK Germany  3
HS Code  29337900

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