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E 2012

Catalog No.GC35921

E 2012 is a potent gamma (γ) secretase modulator without affecting Notch processing.

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E 2012 Chemical Structure

Cas No.: 870843-42-8

Size Price Stock Qty
10mM (in 1mL DMSO)
$123.00
In stock
5mg
$111.00
In stock
10mg
$167.00
In stock
100mg
$1,205.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Description of E 2012

E 2012 is a potent γ-secretase modulator.IC50 value:Target: γ-secretaseIn 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 [1].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 [2].

[1]. Nakano-Ito K, et al. E2012-induced cataract and its predictive biomarkers. Toxicol Sci. 2014 Jan;137(1):249-58. [2]. Portelius E, Van Broeck B, Andreasson U, Gustavsson MK, Mercken M, Zetterberg H, Borghys H, Blennow K.Acute effect on the Aβ isoform pattern in CSF in response to γ-secretase modulator and inhibitor treatment in dogs.J Alzheimers Dis. 2010;21(3):1005-12.

Chemical Properties of E 2012

Cas No. 870843-42-8 SDF
Canonical SMILES O=C(N([C@H](C1=CC=C(C=C1)F)C)CCC/2)C2=C\C3=CC=C(N4C=NC(C)=C4)C(OC)=C3
Formula C25H26FN3O2 M.Wt 419.49
Solubility DMSO: ≥ 50 mg/mL (119.19 mM) Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of E 2012

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1 mg 5 mg 10 mg
1 mM 2.3838 mL 11.9192 mL 23.8385 mL
5 mM 0.4768 mL 2.3838 mL 4.7677 mL
10 mM 0.2384 mL 1.1919 mL 2.3838 mL
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Average Rating: 5 ★★★★★ (Based on Reviews and 23 reference(s) in Google Scholar.)

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