A non-peptide inhibitor of BACE1 (IC50 = 239 nM) that demonstrates ~10-fold selectivity over BACE2 and >50-fold selectivity over other aspartyl proteases; decreases Aβ in APP-overexpressing cells and transgenic animal models and reduces C99 and sAPPβ

LY2811376 – 5 mg

Brand:
Cayman
CAS:
1194044-20-6
Storage:
-20
UN-No:
De Minimis - 3077 / 9

Accumulation of the β-amyloid (Aβ) peptide in the brain is implicated as the primary cause of neurodegeneration and progression of Alzheimer’s disease.{16791} Aβ is derived from sequential proteolytic cleavage of the amyloid precursor protein (APP) by β-secretase (BACE) and γ-secretase.{16790} LY2811376 is a non-peptide inhibitor of BACE1 (IC50 = 239 nM for the synthetic peptide) that demonstrates ~10-fold selectivity over BACE2 and >50-fold selectivity over the aspartyl proteases cathepsin D, pepsin, and renin.{27584} LY2811376 treatment in APP-overexpressing cells and transgenic animal models yields a dose-dependent decrease in Aβ.{27584} Furthermore, LY2811376 has been reported to reduce C99 and sAPPβ, the two primary APP cleavage products generated by BACE1.{27584}  

 

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Description

A non-peptide inhibitor of BACE1 (IC50 = 239 nM) that demonstrates ~10-fold selectivity over BACE2 and >50-fold selectivity over other aspartyl proteases; decreases Aβ in APP-overexpressing cells and transgenic animal models and reduces C99 and sAPPβ, the two primary APP cleavage products generated by BACE1

Formal name: (4S)-4-[2,4-difluoro-5-(5-pyrimidinyl)phenyl]-5,6-dihydro-4-methyl-4H-1,3-thiazin-2-amine

Synonyms: 

Molecular weight: 320.4

CAS: 1194044-20-6

Purity: ≥98%

Formulation: A crystalline solid

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

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