E 2012
E 2012 is a potent gamma (γ) secretase modulator without affecting Notch processing. E 2012 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[1].
Product Specifications
CAS Number
870843-42-8
UNSPSC
12352005
Hazard Statement
H317, H319
Target
γ-secretase
Type
Reference compound
Related Pathways
Neuronal Signaling; Stem Cell/Wnt
Applications
Neuroscience-Neurodegeneration
Field of Research
Neurological Disease
Assay Protocol
https://www.medchemexpress.com/E-2012.html
Purity
97.01
Solubility
DMSO : 50 mg/mL (ultrasonic)
Smiles
O=C(N([C@H](C1=CC=C(C=C1)F)C)CCC/2)C2=C\C3=CC=C(N4C=NC(C)=C4)C(OC)=C3
Molecular Formula
C25H26FN3O2
Molecular Weight
419.49
Precautions
H317, H319
References & Citations
[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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Phase 1
Available Sizes
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