851600-86-7

Name	N-[(4-bromophenyl)methyl]-4-chloro-N-[(3R)-hexahydro-2-oxo-1H-azepin-3-yl]-Benzenesulfonamide
CAS	851600-86-7
Molecular Formula	C19H20BrClN2O3S
MDL Number	MFCD13184809
Molecular Weight	471.801
MOL File	851600-86-7.mol

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

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Chemical Properties

form	Solid
color	Off-white to light yellow

Hazard Information

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

Supplier

ChemeGen(Shanghai) Biotechnology Co.,Ltd.

Telephone 18818260767

Websitehttp://www.chemegen.com

RD International Technology Co., Limited

Telephone 18024082417

Websitehttps://www.ruidiresearch.com

TargetMol Chemicals Inc.

Telephone 15002134094

Websitehttps://www.targetmol.cn/

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