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

E 2012 

Cat. No.: HY-10016 Purity: 96.91%
Handling Instructions

E 2012 is a potent γ-secretase modulator.

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

E 2012 Chemical Structure

E 2012 Chemical Structure

CAS No. : 870843-42-8

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 515 In-stock
Estimated Time of Arrival: December 31
5 mg USD 468 In-stock
Estimated Time of Arrival: December 31
10 mg USD 678 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2345 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

    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
    • Biological Activity

    • Technical Information

    • Purity & Documentation

    • References

    Description

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

    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    90% (20% SBE-β-CD in saline)

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

    • 2.

      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

    • 3.

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

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

    References
    Molecular Weight

    419.49

    Formula

    C₂₅H₂₆FN₃O₂

    CAS No.

    870843-42-8

    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

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

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    Product Name:
    E 2012
    Cat. No.:
    HY-10016
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    E 2012

    Cat. No.: HY-10016