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E 2012

Catalog No. T15184   CAS 870843-42-8

E2012 is a γ-secretase modulator (GSM). E2012 inhibits 3β-hydroxysterol Δ24-reductase (DHCR24) at the final step in the cholesterol biosynthesis. E 2012 aims at Alzheimer's disease by reduction of amyloid β-42, and induces cataract following repeated doses in the rat.

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E 2012 Chemical Structure
E 2012, CAS 870843-42-8
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1 mg In stock $ 34.00
2 mg In stock $ 48.00
5 mg In stock $ 80.00
10 mg In stock $ 122.00
25 mg In stock $ 198.00
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Purity: 99.83%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description E2012 is a γ-secretase modulator (GSM). E2012 inhibits 3β-hydroxysterol Δ24-reductase (DHCR24) at the final step in the cholesterol biosynthesis. E 2012 aims at Alzheimer's disease by reduction of amyloid β-42, and induces cataract following repeated doses in the rat.
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[1].
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[2].
Molecular Weight 419.49
Formula C25H26FN3O2
CAS No. 870843-42-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 50 mg/mL (119.19 mM)

TargetMolReferences and Literature

1. Nakano-Ito K, et al. E2012-induced cataract and its predictive biomarkers. Toxicol Sci. 2014 Jan;137(1):249-58. 2. Portelius E, Van Broeck B, Andreasson U, Gustavsson MK, Mercken M, Zetterberg H, Borghys H, Blennow K.Acute effect on the Aβ isoform pattern in CSF in response to γ-secretase modulator and inhibitor treatment in dogs.J Alzheimers Dis. 2010;21(3):1005-12.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Neurodegenerative Disease Compound Library Neuronal Signaling Compound Library ReFRAME Related Library Protease Inhibitor Library Stem Cell Differentiation Compound Library Bioactive Compounds Library Max Anti-Alzheimer's Disease Compound Library Bioactive Compound Library NO PAINS Compound Library

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Keywords

E 2012 870843-42-8 Neuroscience Proteases/Proteasome Stem Cells Gamma-secretase γ-secretase inhibit E2012 E-2012 Inhibitor Gamma secretase inhibitor

 

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