1. Neuronal Signaling
    Stem Cell/Wnt
  2. γ-secretase
  3. E 2012

E 2012 

Cat. No.: HY-10016 Purity: 97.39%
Handling Instructions

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.

For research use only. We do not sell to patients.

E 2012 Chemical Structure

E 2012 Chemical Structure

CAS No. : 870843-42-8

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Solution
10 mM * 1 mL in DMSO USD 110 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 110 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 100 In-stock
Estimated Time of Arrival: December 31
10 mg USD 150 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1100 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 6 publication(s) in Google Scholar

Top Publications Citing Use of Products

    E 2012 purchased from MCE. Usage Cited in: Cell Rep. 2015 May 5;11(5):689-96.

    Western blots performed on soluble protein extracts of neurons following treatment with the indicated compounds. Protein extraction performed at day 90 post-neural induction, after 30 days of drug treatment. DAPT treatment (GSI) increases both total and phosphorylated tau expression in the majority of genotypes, assessed at multiple epitopes. By contrast, E2012 (GSM) reduces total tau expression and its phosphorylation in all genotypes assayed, with particularly pronounced effects in Ts21 neuron
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    Description

    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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Molecular Weight

    419.49

    Formula

    C₂₅H₂₆FN₃O₂

    CAS No.
    SMILES

    O=C(N([[email protected]](C1=CC=C(C=C1)F)C)CCC/2)C2=C\C3=CC=C(N4C=NC(C)=C4)C(OC)=C3

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 50 mg/mL (119.19 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 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
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: 2.5 mg/mL (5.96 mM); Clear solution; Need ultrasonic

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: 2.5 mg/mL (5.96 mM); Clear solution; Need ultrasonic

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (5.96 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
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    Keywords:

    E 2012E2012E-2012γ-secretaseGamma secretaseInhibitorinhibitorinhibit

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