E-2012

Biological Activity

E 2012 is a potent γ-secretase modulator. In the present study, 9 dogs were treated with a single dose of the γ-secretase modulator E2012, the γ-secretase inhibitor LY450139, or vehicle with a dosing interval of 1 week. The isoform Aβ(1-37) was significantly increased in a dose-dependent manner in response to treatment with E2012, while Aβ(1-39), Aβ(1-40) and A(1-42) decreased. E2012, a gamma secretase modulator without affecting Notch processing, aimed at Alzheimer's disease by reduction of amyloid β-42, induced cataract following repeated doses in the rat.E2012 inhibits 3β-hydroxysterol Δ24-reductase (DHCR24) at the final step in the cholesterol biosynthesis. In vivo lenticular concentration of E2012 after 13-week repeated dose with cataract was well above those where inhibition was observed in vitro.E2012 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. For the detailed information of E-2012, the solubility of E-2012 in water, the solubility of E-2012 in DMSO, the solubility of E-2012 in PBS buffer, the animal experiment (test) of E-2012, the cell expriment (test) of E-2012, the in vivo, in vitro and clinical trial test of E-2012, the EC50, IC50,and affinity,of E-2012, For the detailed information of E-2012, the solubility of E-2012 in water, the solubility of E-2012 in DMSO, the solubility of E-2012 in PBS buffer, the animal experiment (test) of E-2012, the cell expriment (test) of E-2012, the in vivo, in vitro and clinical trial test of E-2012, the EC50, IC50,and affinity,of E-2012, Please contact DC Chemicals.

Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.