E 2012

SKU: orb1308359

Description

E 2012

Research Area

Neuroscience, Protein Biochemistry, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 870843-42-8
• MW: 419.49
• Purity: 99.83%
• Formula: C₂₅H₂₆FN₃O₂
• SMILES: COc1cc(\C=C2/CCCN([C@@H](C)c3ccc(F)cc3)C2=O)ccc1-n1cnc(C)c1
• Target: Gamma-secretase
• Solubility: DMSO:50 mg/mL (119.19 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.77 mM)

Bioactivity

• In Vivo:
  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 CSF Aβ isoform pattern was analyzed by immunoprecipitation combined with MALDI-TOF mass spectrometry. Aβ(1-15) and Aβ(1-16) increase while Aβ(1-34) decreases in response to treatment with the γ-secretase inhibitor LY450139, which is in agreement with previous studies. 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. The data presented suggests that the γ-secretase modulator E-2012 alters the cleavage site preference of γ-secretase. The increase in Aβ(1-37) may inhibit Aβ(1-42) oligomerization and toxicity.
• In Vitro:
  In vitro studies to investigate the effect of E2012 on cholesterol metabolism demonstrated that E2012 inhibits 3β-hydroxysterol Δ24-reductase (DHCR24) at the final step in the cholesterol biosynthesis.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

γ-secretase, γ secretase, inhibit, Inhibitor, Gamma secretase, Gammasecretase, E 2012, E2012, E-2012

Compound Identifiers

PubChem CID

11560787