ELN318463ELN318463
MedChemExpress (MCE)
HY-50882
851600-86-7
99.45%
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Room temperature in continental US
may vary elsewhere.
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.
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].
EC50: 12 nM (PS1 γ-secretase), 656 nM (PS2 γ-secretase)[1] In Vitro 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]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> ELN318463 Related Antibodies
| | | |
| | | | | |
[1]. Zhao B, et al. Identification of gamma-secretase inhibitor potency determinants on presenilin. J Biol Chem. 2008 Feb 1
283(5):2927-38. [Content Brief]
[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. [Content Brief]