Avagacestat
Chemical Name: (2R)-2-[[(4-Chlorophenyl)sulfonyl][[2-fluoro-4-(1,2,4-oxadiazol-3-yl)phenyl]methyl]amino]-5,5,5-trifluoropentanamide
Purity: ≥98%
Biological Activity
Avagacestat is a highly potent γ-secretase inhibitor (Aβ40 IC50 = 0.3 nM). Exhibits >137-fold selectivity for amyloid-β precursor protein (APP) processing over Notch. Reduces plasma and brain Aβ40 and Aβ42 levels in vivo. Orally bioavailable.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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Discovery and evaluation of BMS-708163, a potent, selective and orally bioavailable γ-secretase inhibitor.
Gillman et al.
ACS Med.Chem.Lett., 2010;1:120 -
Pharmacodynamics of selective inhibition of γ-secretase by avagacestat.
Albright et al.
J.Pharmacol.Exp.Ther., 2013;344:686
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Citation for Avagacestat
The citations listed below are publications that use Tocris products. Selected citations for Avagacestat include:
1 Citation: Showing 1 - 1
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Roles for ADAM17 in TNF-R1 Mediated Cell Death and Survival in Human U937 and Jurkat Cells.
Authors: Wulf Et al.
Cells 2021;10
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