Description
BMS-708163 (Avagacestat) can inhibit Abeta42, Abeta40, and Abeta38 with IC50 of 0.79 nM, 0.78 nM and 0.66 nM.
Storage
2 years at -20 centigrade
Targets
Abeta42, Abeta40, Abeta38
Molecular Formula
C20H17ClF4N4O4S
Chemical Name
(2R)-2-(N-(2-fluoro-4-(1,2,4-oxadiazol-3-yl)benzyl)-4-chlorophenylsulfonamido)-5,5,5-trifluoropentanamide
Solubility
DSMO 104 mg/mL Water
In vitro
BMS-708163, (R)-2-(4-chloro-N-(2-fluoro-4- (1,2,4-oxadiazol-3-yl)benzyl) phenylsulfonamido)-5,5,5-trifluor-opentanamide, is a novel, sulfonamide containing gamma -secretase inhibitor. BMS-708163 showed potent A beta 40 inhibition (1.4 nM) and >300-fold selectivity versus Notch (540 nM).
In vivo
Orally administered to Tg2576 mice (aged 5.5 months )for 8d. BMS-708163 significantly ameliorated cognitive deficits in Tg2576 mice on day 1, but not on day 8.
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