| Identification | Back Directory | [Name]
N-[(4-bromophenyl)methyl]-4-chloro-N-[(3R)-hexahydro-2-oxo-1H-azepin-3-yl]-Benzenesulfonamide | [CAS]
851600-86-7 | [Synonyms]
ELN 318463
ELN318463,ELN-318463
N-[(4-bromophenyl)methyl]-4-chloro-N-[(3R)-2-oxoazepan-3-yl]benzenesulfonamide
N-[(4-bromophenyl)methyl]-4-chloro-N-[(3R)-hexahydro-2-oxo-1H-azepin-3-yl]-Benzenesulfonamide | [Molecular Formula]
C19H20BrClN2O3S | [MDL Number]
MFCD13184809 | [MOL File]
851600-86-7.mol | [Molecular Weight]
471.801 |
| Hazard Information | Back Directory | [Uses]
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 12 nM and 656 nM for PS1 and PS2, respectively. ELN318463 is 51-fold more selective for PS1[1][2]. | [in vivo]
ELN318463 (30 mg/kg or 100 mg/kg; orally) leads acute reduction of brain Aβ in in the PDAPP transgene model of Alzheimer's disease (AD) as well as in wild-type FVB strain mice[2]. | Animal Model: | Female, two- to three-month old, FVB/N mice and PDAPP transgene model of Alzheimer's disease (AD)[2] | | Dosage: | 30 mg/kg or 100 mg/kg | | Administration: | Orally | | Result: | Brain levels at 30 mg/kg were 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. |
| [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 |
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