| Identification | Back Directory | [Name]
ELN 318463 (racemate) | [CAS]
851599-82-1 | [Synonyms]
ELN 318463 (racemate)
N-[(4-bromophenyl)methyl]-4-chloro-N-(2-oxoazepan-3-yl)benzenesulfonamide
Benzenesulfonamide, N-[(4-bromophenyl)methyl]-4-chloro-N-(hexahydro-2-oxo-1H-azepin-3-yl)- | [Molecular Formula]
C19H20BrClN2O3S | [MOL File]
851599-82-1.mol | [Molecular Weight]
471.8 |
| Hazard Information | Back Directory | [Uses]
ELN318463 racemate is the racemate of ELN318463. ELN318463 is an amyloid precursor protein (APP) selective γ-secretase inhibitor. ELN318463 shows differential inhibition of presenilin (PS1)- and PS2-comprised γ-secretase with EC50s of 12nM and 656 nM for PS1and PS2, respectively. ELN318463 is 51-fold more selective for PS1[1][2]. | [in vivo]
Brain levels of ELN318463 at 30 mg/kg are 0.754 μM in FVB brains and 0.69 μM in PDAPP brains, and at 100 mg/kg dose the levels were 2.7 μM in FVB brains and 1.87 μM in PDAPP brains. Discordance between Aβ1-40 and Aβx-40 in BACE KO or wild-type BACE inhibitor treated mice has been reported[1]. | [References]
[1] Zhao B, et al. Identification of gamma-secretase inhibitor potency determinants on presenilin. J Biol Chem. 2008 Feb 1;283(5):2927-38. DOI:10.1074/jbc.M708870200
[2] Basi GS, et al. Amyloid precursor protein selective gamma-secretase inhibitors for treatment of Alzheimer's disease. Alzheimers Res Ther. 2010 Dec 29;2(6):36. DOI:10.1186/alzrt60 |
|
|