For research use only. Not for therapeutic Use.
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].
ELN318463 behaves as a classic γ-secretase inhibitor, demonstrates 75- to 120-fold selectivity for inhibiting Aβ production compared with Notch signaling in cells, and displaces an active site directed inhibitor at very high concentrations only in the presence of substrate[2].
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].
| Catalog Number | I015568 |
| CAS Number | 851600-86-7 |
| Synonyms | N-[(4-bromophenyl)methyl]-4-chloro-N-[(3R)-2-oxoazepan-3-yl]benzenesulfonamide |
| Molecular Formula | C19H20BrClN2O3S |
| Purity | ≥95% |
| InChI | InChI=1S/C19H20BrClN2O3S/c20-15-6-4-14(5-7-15)13-23(18-3-1-2-12-22-19(18)24)27(25,26)17-10-8-16(21)9-11-17/h4-11,18H,1-3,12-13H2,(H,22,24)/t18-/m1/s1 |
| InChIKey | KTCJYACFOQWRDO-GOSISDBHSA-N |
| SMILES | C1CCNC(=O)C(C1)N(CC2=CC=C(C=C2)Br)S(=O)(=O)C3=CC=C(C=C3)Cl |
| Reference | [1]. Zhao B, et al. Identification of gamma-secretase inhibitor potency determinants on presenilin. J Biol Chem. 2008 Feb 1;283(5):2927-38. [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. |
