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Description: γ-secretase modulator; Notch-sparing
Chemical Name: (3E)-1-[(1S)-1-(4-Fluorophenyl)ethyl]-3-[[3-methoxy-4-(4-methyl-1H-imidazol-1-yl)phenyl]methylene]-2-piperidone
Purity: ≥98% (HPLC)
Biological Activity for E 2012
E 2012 is a γ-secretase modulator. Lowers Aβ40 and Aβ42 levels and increases Aβ37 levels, in vitro and in vivo. Displays no effect on γ-secretase processing of Notch, EphA4 and EphB2.
Compound Libraries for E 2012
E 2012 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for E 2012
| M. Wt | 419.49 |
| Formula | C25H26FN3O2 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 870843-42-8 |
| PubChem ID | 11560787 |
| InChI Key | PUOAETJYKQITMO-LANLRWRYSA-N |
| Smiles | COC1=C(N2C=C(C)N=C2)C=CC(/C=C3CCCN([C@@H](C)C4=CC=C(F)C=C4)C\3=O)=C1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for E 2012
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| 1eq. HCl | 41.95 | 100 | |
| DMSO | 41.95 | 100 |
Preparing Stock Solutions for E 2012
The following data is based on the product molecular weight 419.49. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.38 mL | 11.92 mL | 23.84 mL |
| 5 mM | 0.48 mL | 2.38 mL | 4.77 mL |
| 10 mM | 0.24 mL | 1.19 mL | 2.38 mL |
| 50 mM | 0.05 mL | 0.24 mL | 0.48 mL |
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Product Datasheets for E 2012
References for E 2012
References are publications that support the biological activity of the product.
Borgegard et al (2012) First and second generation γ-secretase modulators (GSMs) modulate amyloid-β (Aβ) peptide production through different mechanisms. J.Biol.Chem. 287 15 PMID: 22334705
Portelius et al (2010) Acute effect on the Aβ isoform pattern in CSF in response to γ-secretase modulator and inhibitor treatment in dogs. J.Alzheimers Dis. 21 1005 PMID: 20634579
If you know of a relevant reference for E 2012, please let us know.
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Citations for E 2012
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