YO-01027 , ≥97% , 209984-56-5

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

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
• pka: 12.76±0.20(Predicted)
• form: White solid
• color: white to beige
• optical activity: [α]/D -128.0 to -154.0°-0.25 in methanol
• 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