| Name | E 2012 |
| 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]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 50 mg/mL (119.19 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (4.77 mM), Sonication is recommended.
|
| Keywords | γ-secretase | γ secretase | Inhibitor | inhibit | Gammasecretase | Gamma secretase | E-2012 | E2012 | E 2012 |
| Inhibitors Related | Valproic acid sodium salt | Aβ42-IN-2 | Sulindac sulfide | Tangeretin | gamma-secretase modulator 1 | Valproic Acid | Hexamethylene bisacetamide | CB-103 | Prednisone acetate | Carvacrol | RO7185876 | DAPT |
| Related Compound Libraries | Anti-Neurodegenerative Disease Compound Library | Bioactive Compound Library | Neuronal Signaling Compound Library | Anti-Alzheimer's Disease Compound Library | ReFRAME Related Library | Protease Inhibitor Library | NO PAINS Compound Library | Stem Cell Differentiation Compound Library | Bioactive Compounds Library Max | Fluorochemical Library |
United States
