A γ-secretase modulator
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E2012

Item No. 29710

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(3E)-1-[(1S)-1-(4-fluorophenyl)ethyl]-3-[[3-methoxy-4-(4-methyl-1H-imidazol-1-yl)phenyl]methylene]-2-piperidinone
CAS Number
870843-42-8
Molecular Formula
C25H26FN3O2
Formula Weight
419.5
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMF: 10mg/mLDMSO: 10mg/mLDMSO:PBS (pH 7.2) (1:3): 0.25mg/mLEthanol: 10mg/mL
λmax
286 nm
SMILES
FC1=CC=C([C@H](C)N2C(/C(CCC2)=C/C3=CC(OC)=C(N4C=NC(C)=C4)C=C3)=O)C=C1
InChi Code
InChI=1S/C25H26FN3O2/c1-17-15-28(16-27-17)23-11-6-19(14-24(23)31-3)13-21-5-4-12-29(25(21)30)18(2)20-7-9-22(26)10-8-20/h6-11,13-16,18H,4-5,12H2,1-3H3/b21-13+/t18-/m0/s1
InChi Key
PUOAETJYKQITMO-LANLRWRYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
Certificates of Analysis & Batch Specific Data

Provide batch numbers separated by commas to download or request available product inserts, QC sheets, certificates of analysis, data packs, and GC-MS data.

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    5 mg

    $107

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    10 mg

    $193

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    25 mg

    $451

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    50 mg

    $845

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    Product Description

    E2012 is a modulator of γ-secretase.1 It selectively inhibits APP intracellular signaling domain (AICD) cleavage to amyloid-β (Aβ) over Notch cleavage to its signaling effector Notch intracellular domain (NICD), processes both mediated by γ-secretase, when used at a concentration of 1 µM in luciferase assays.2 E2012 also inhibits the activity of the cholesterol synthesis enzyme 3β-hydroxysterol ∆24-reductase (DHCR24) in primary rat hepatocytes and HepG2 cells (IC50s = 11 and 15 nM, respectively).3 It reduces Aβ (1-42) (Aβ42) production in primary rat embryonic cerebral cortex neurons with an IC50 value of 220 nM.4 E2012 (100 mg/kg) also decreases Aβ42 levels in guinea pig brain and cerebral spinal fluid (CSF).4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Hahn, S., Brüning, T., Ness, J., et al. Presenilin-1 but not amyloid precursor protein mutations present in mouse models of Alzheimer’s disease attenuate the response of cultured cells to γ-secretase modulators regardless of their potency and structure. J. Neurochem. 116(3), 385-395 (2011).

    2. Dimitrov, M., Alattia, J.-R., Lemmin, T., et al. Alzheimer’s disease mutations in APP but not γ-secretase modulators affect epsilon-cleavage-dependent AICD production. Nat. Commun. 4:2246, (2013).

    3. Nakano-Ito, K., Fujikawa, Y., Hihara, T., et al. E2012-induced cataract and its predictive biomarkers. Toxicol. Sci. 137(1), 249-258 (2014).

    4. Kimura, T., Kawano, K., Doi, E., et al. Cinnamide compound. (2005).