E 2012


CAS No. : 870843-42-8

870843-42-8
Price and Availability of CAS No. : 870843-42-8
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Cat. No. : HY-10016
M.Wt: 419.49
Formula: C25H26FN3O2
Purity: >98 %
Solubility: DMSO : ≥ 50 mg/mL (119.19 mM)
Introduction of 870843-42-8 :

E 2012 is a potent gamma (γ) secretase modulator without affecting Notch processing. E 2012 inhibits 3β-hydroxysterol Δ24-reductase (DHCR24) at the final step in the cholesterol biosynthesis. E 2012 aims at Alzheimer's disease by reduction of amyloid β-42, and induces cataract following repeated doses in the rat[1]. In Vitro: 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[1]. In Vivo: 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[2].

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