E-2012

Research use only, not for human use.

A potent, second-generation γ-secretase modulator that decreases Aβ(1-39), Aβ(1-40) and A(1-42), and increases Aβ(1-37).

A potent, second-generation γ-secretase modulator that decreases Aβ(1-39), Aβ(1-40) and A(1-42), and increases Aβ(1-37).Alzheimer's Disease Discontinued.

E2012 has concentration-dependent inhibitory effects on cholesterol biosynthesis in primary culture of rat hepatocytes and HepG2 cells with IC50s of 11.0, and 15.1 nM, respectively.

In vivo lenticular concentration of E 2012 after 13-week repeated dose with cataract was well above those where inhibition is observed in vitro. E 2012 induces cataract in the rat by inhibiting DHCR24 at the final step of cholesterol synthesis with associated elevation in desmosterol within the lens, preceded by desmosterol changes that would serve as a predictive safety biomarker for lenticular opacity.

E2012

Wnt/Notch/Hedgehog

γ-secretase

γ-secretase

Neurological Disease

Alzheimer Disease

870843-42-8

419.4912

C25H26FN3O2

>98% (HPLC)

10 mM in DMSO

O=C1N([C@H](C2=CC=C(F)C=C2)C)CCC/C1=C\C3=CC=C(N4C=C(C)N=C4)C(OC)=C3

2-Piperidinone, 1-[(1S)-1-(4-fluorophenyl)ethyl]-3-[[3-methoxy-4-(4-methyl-1H-imidazol-1-yl)phenyl]methylene]-, (3E)-

(-20℃)

With Ice Pack

≥ 2 years