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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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