E 2012
(E)-1-[(1S)-1-(4-Fluorophenyl)ethyl]-3-[3-methoxy-4-(4-methyl-1H-imidazol-1-yl)benzylidene]piperidin-2-one
CAS: 870843-42-8
Molecular Formula: C25H26FN3O2
E 2012 - Names and Identifiers
E 2012 - Physico-chemical Properties
| Molecular Formula | C25H26FN3O2 |
| Molar Mass | 419.49 |
| Density | 1.19±0.1 g/cm3(Predicted) |
| Boling Point | 649.2±55.0 °C(Predicted) |
| pKa | 5.67±0.61(Predicted) |
| Storage Condition | 2-8℃ |
| In vitro study | E2012 has concentration-dependent inhibitory effects on cholesterol biosynthesis in primary culture of rat hepatocytes and HepG2 cells with IC 50 s of 11.0, and 15.1 nM, respectively. |
| In vivo study | In vivo lenticular concentration of E 2012 after 13-week repeated dose with cataract was well above those where inhibition is observed in vitro. E 2012 induces cataract in the rat by inhibiting DHCR24 at the final step of cholesterol synthesis with associated elevation in desmosterol within the lens, preceded by desmosterol changes that would serve as a predictive safety biomarker for lenticular opacity. |
E 2012 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.384 ml | 11.919 ml | 23.838 ml |
| 5 mM | 0.477 ml | 2.384 ml | 4.768 ml |
| 10 mM | 0.238 ml | 1.192 ml | 2.384 ml |
| 5 mM | 0.048 ml | 0.238 ml | 0.477 ml |
Last Update：2024-01-02 23:10:35
E 2012 - Reference Information
| biological activity | E 2012 is an effective gamma secretase regulator and will not affect Notch processing. E 2012 inhibits 3 β-hydroxysterol Δ24-reductase (DHCR24) in the last step of cholesterol biosynthesis. E 2012 was designed to reduce Alzheimer's disease by reducing amyloid β-42 and to induce cataracts after repeated dosing in rats. |
| in vitro study | E2012 has concentration-dependent inhibitory effects on cholesterol biosynthesis in primary culture of rat hepatocytes and HepG2 cells with IC 50 s of 11.0, and 15.1 nM, respectively. |
| in vivo research | in vivo lenticular concentration of E 2012 after 13-week repeated dose with cataract was well above where inhibition is observed in vitro. E 2012 induces cataract in the rat by inhibiting DHCR24 at the final step of cholesterol synthesis with associated elevation in desmosterol within the lens, preceded by desmosterol changes that would serve as a predictive safety biomarker for lenticular opacity. |
Last Update：2024-04-09 15:16:39
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CAS: 870843-42-8
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Product Name: (E)-1-[(1S)-1-(4-Fluorophenyl)ethyl]-3-[3-methoxy-4-(4-methyl-1H-imidazol-1-yl)benzylidene]piperidin-2-one Visit Supplier Webpage Request for quotation
CAS: 870843-42-8
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
CAS: 870843-42-8
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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