An inhibitor of γ-secretase (IC50s = 6.2 and 1.2 nM

PF-3084014 – 5 mg

Brand:
Cayman
CAS:
1290543-63-3
Storage:
-20
UN-No:
De Minimis - 3077 / 9

PF-3084014 is a γ-secretase inhibitor (IC50s = 6.2 and 1.2 nM in an enzyme assay and in whole cells, respectively).{45150} It inhibits γ-secretase activity without inducing Notch-related toxicity (EC50s = 1,300-3,000 nM for B cells in fetal thymic organ cultures). It reduces the level of amyloid-β (1-40) (Aβ40) fragments in mouse brain three hours following administration of 1 to 18 mg/kg doses and reduces Aβ42 fragment levels when administered at doses of 9 or 18 mg/kg. It also reduces Aβ fragments in guinea pig brain when administered at doses ranging from 0.3 to 3 mg/kg per day for five days.  

 

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SKU: 27061 - 5 mg Category:

Description

An inhibitor of γ-secretase (IC50s = 6.2 and 1.2 nM, respectively, in an enzyme assay and in whole cells); does not induce Notch-related toxicity (EC50s = 1,300-3,000 nM for B cells in fetal thymic organ cultures); reduces the level of Aβ40 fragments in mouse brain three hours following 1 to 18 mg/kg doses and the level of Aβ42 fragments levels at 9 or 18 mg/kg; reduces Aβ fragments when at 0.3-3 mg/kg per day for five days

Formal name: (2S)-2-[[(2S)-6,8-difluoro-1,2,3,4-tetrahydro-2-naphthalenyl]amino]-N-[1-[2-[(2,2-dimethylpropyl)amino]-1,1-dimethylethyl]-1H-imidazol-4-yl]-pentanamide

Synonyms: 

Molecular weight: 489.6

CAS: 1290543-63-3

Purity: ≥98%

Formulation: A solid

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

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