An inhibitor of γ-secretase (IC50 = 15 nM for AAP cleavage to Aβ40); 14-fold selective for γ-secretase over Notch-1; reduces brain levels of Aβ40 and Aβ42 in the Tg2576 transgenic mouse model of Alzheimer's disease; also increases contextual fear conditioning freezing time in Tg2576 mice

Begacestat – 1 mg

Brand:
Cayman
CAS:
769169-27-9
Storage:
-20
UN-No:
Non-Hazardous - /

Begacestat is an inhibitor of γ-secretase that inhibits cleavage of amyloid precursor protein (APP) to amyloid-β (1-40) (Aβ40; Item No. 21617) in vitro (IC50 = 15 nM).{35876} It is 14-fold selective for γ-secretase over Notch-1. Begacestat (5 mg/kg) reduces brain levels of Aβ40 and Aβ42 (Item No. 20574) in the Tg2576 transgenic mouse model of Alzheimer’s disease. It also increases contextual fear conditioning freezing time, indicating reversal of contextual memory deficits, in Tg2576 mice in a dose-dependent manner.{48451}  

 

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SKU: 27916 - 1 mg Category:

Description

An inhibitor of γ-secretase (IC50 = 15 nM for AAP cleavage to Aβ40); 14-fold selective for γ-secretase over Notch-1; reduces brain levels of Aβ40 and Aβ42 in the Tg2576 transgenic mouse model of Alzheimer’s disease; also increases contextual fear conditioning freezing time in Tg2576 mice

Formal name: 5-chloro-N-[(1S)-3,3,3-trifluoro-1-(hydroxymethyl)-2-(trifluoromethyl)propyl]-2-thiophenesulfonamide

Synonyms:  GSI-953

Molecular weight: 391.7

CAS: 769169-27-9

Purity: ≥98%

Formulation: A solid

Product Type|Biochemicals|Small Molecule Inhibitors|Peptidases & Proteases||Research Area|Neuroscience|Behavioral Neuroscience|Learning & Memory||Research Area|Neuroscience|Neurodegenerative Disorders|Alzheimer’s Disease

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