E 2012

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Cat.No. 5550 - E 2012 | C25H26FN3O2 | CAS No. 870843-42-8
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)
Datasheet
Citations
Reviews
Literature

Biological Activity

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.

Technical Data

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

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
1eq. HCl 41.95 100
DMSO 41.95 100

Preparing Stock Solutions

The following data is based on the product molecular weight 419.49. Batch specific molecular weights may vary from batch to batch due to solvent 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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References

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


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