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 EC 50 s of 12 nM and 656 nM for PS1 and PS2, respectively. ELN318463 is 51-fold more selective for PS1 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Female, two- to three-month old, FVB/N mice and PDAPP transgene model of Alzheimer's disease (AD)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. Form:Solid IC50& Target:EC50: 12 nM (PS1 γ-secretase), 656 nM (PS2 γ-secretase)

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