E 2012
Based on 7 publication(s) in Google Scholar
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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 97.01%
- No. CAS: 870843-42-8
- Fòrmula: C25H26FN3O2
- Peso molecular:419.49
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) E 2012
More- Cell. 2021 Jan 21;184(2):521-533.e14. [Abstract]
- Nat Commun. 2013;4:2246. [Abstract]
- Cell Rep. 2015 May 5;11(5):689-96. [Abstract]
- Stem Cell Reports. 2017 Apr 11;8(4):870-882. [Abstract]
- J Neurochem. 2013 May;125(4):610-9. [Abstract]
- Reprod Domest Anim. 2022 Jan;57(1):10-18. [Abstract]
- bioRxiv. 2024 September 13.
Customer Validation & Images
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Actividad biológica
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
143 nM
Compound: 1, E2012
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Inhibition of gamma secretase expressed in CHO cells expressing APP assessed as amyloid beta42 production
Inhibition of gamma secretase expressed in CHO cells expressing APP assessed as amyloid beta42 production
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[PMID: 22429469] |
| HEK293 | IC50 |
64 nM
Compound: Eisai
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Inhibition of gamma secretase-mediated amyloid beta42 production in HEK293 cells
Inhibition of gamma secretase-mediated amyloid beta42 production in HEK293 cells
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[PMID: 20724152] |
| HEK293 | IC50 |
64 nM
Compound: 1
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Inhibition of gamma secretase-mediated amyloid beta42 production in HEK293 cells by sandwich immunoassay
Inhibition of gamma secretase-mediated amyloid beta42 production in HEK293 cells by sandwich immunoassay
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[PMID: 21195610] |
| HEK293 | IC50 |
2300 nM
Compound: 1, E-2012
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Modulation of gamma-secretase-mediated cleavage of human APP Swedish and London mutation expressed in HEK293 cells assessed as inhibition of amyloid beta40 production after 5 hrs by sandwich immunoassay
Modulation of gamma-secretase-mediated cleavage of human APP Swedish and London mutation expressed in HEK293 cells assessed as inhibition of amyloid beta40 production after 5 hrs by sandwich immunoassay
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[PMID: 22098494] |
| HEK293 | IC50 |
64 nM
Compound: 1, E-2012
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Modulation of gamma-secretase-mediated cleavage of human APP Swedish and London mutation expressed in HEK293 cells assessed as inhibition of amyloid beta42 production after 5 hrs by sandwich immunoassay
Modulation of gamma-secretase-mediated cleavage of human APP Swedish and London mutation expressed in HEK293 cells assessed as inhibition of amyloid beta42 production after 5 hrs by sandwich immunoassay
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[PMID: 22098494] |
| HEK293 | IC50 |
14 μM
Compound: 1, E-2012
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Modulation of gamma-secretase-mediated cleavage of human APP Swedish and London mutation expressed in HEK293 cells assessed as reduction of total amyloid beta level after 5 hrs by sandwich immunoassay
Modulation of gamma-secretase-mediated cleavage of human APP Swedish and London mutation expressed in HEK293 cells assessed as reduction of total amyloid beta level after 5 hrs by sandwich immunoassay
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[PMID: 22098494] |
| HEK293 | IC50 |
0.16 μM
Compound: 3, E2012
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Modulation of gamma-secretase in HEK293 cells expressing guinea pig Swedish mutant SFV-APP695sw assessed as inhibition of amyloid beta-42 production after 16 to 18 hrs by HTRF assay
Modulation of gamma-secretase in HEK293 cells expressing guinea pig Swedish mutant SFV-APP695sw assessed as inhibition of amyloid beta-42 production after 16 to 18 hrs by HTRF assay
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[PMID: 24139583] |
| HEK293 | IC50 |
560 nM
Compound: E2012
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Modulation of gamma-secretase in HEK293 cells expressing Swedish mutant APP assessed as inhibition of intracellular amyloid beta 40 production after 16 hrs by sandwich ELISA
Modulation of gamma-secretase in HEK293 cells expressing Swedish mutant APP assessed as inhibition of intracellular amyloid beta 40 production after 16 hrs by sandwich ELISA
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[PMID: 26142947] |
| HEK293 | IC50 |
85 nM
Compound: E2012
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Modulation of gamma-secretase in HEK293 cells expressing Swedish mutant APP assessed as inhibition of intracellular amyloid beta 42 production after 16 hrs by sandwich ELISA
Modulation of gamma-secretase in HEK293 cells expressing Swedish mutant APP assessed as inhibition of intracellular amyloid beta 42 production after 16 hrs by sandwich ELISA
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[PMID: 26142947] |
| HEK293 | IC50 |
64 nM
Compound: 2
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Modulation of gamma secretase in HEK293 cells transfected with human APP with Swedish and London familial AD mutation assessed as reduction in Abeta42 levels incubated for 5 hrs by sandwich immuno-assay
Modulation of gamma secretase in HEK293 cells transfected with human APP with Swedish and London familial AD mutation assessed as reduction in Abeta42 levels incubated for 5 hrs by sandwich immuno-assay
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[PMID: 32786237] |
E2012 has concentration-dependent inhibitory effects on cholesterol biosynthesis in primary culture of rat hepatocytes and HepG2 cells with IC50s of 11.0, and 15.1 nM, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 870843-42-8
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Appearance Solid
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Peso molecular 419.49
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Fòrmula C25H26FN3O2
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Color Light yellow to yellow
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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
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (7)
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Journal Impact Factor
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Most Recent
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Cell
2021 Jan 21;184(2):521-533.e14. PMID: 33373587 -
Nat Commun
Alzheimer's disease mutations in APP but not γ-secretase modulators affect epsilon-cleavage-dependent AICD production. [Abstract]2013;4:2246. PMID: 23907250 -
Cell Rep
2015 May 5;11(5):689-96. PMID: 25921538
E 2012 purchased from MedChemExpress. Usage Cited in: Cell Rep. 2015 May 5;11(5):689-96. [Abstract]
Western blots performed on soluble protein extracts of neurons following treatment with the indicated compounds. Protein extraction performed at day 90 post-neural induction, after 30 days of drug treatment. DAPT treatment (GSI) increases both total and phosphorylated tau expression in the majority of genotypes, assessed at multiple epitopes. By contrast, E2012 (GSM) reduces total tau expression and its phosphorylation in all genotypes assayed, with particularly pronounced effects in Ts21 neuron
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Stem Cell Reports
Phenotypic Screening Identifies Modulators of Amyloid Precursor Protein Processing in Human Stem Cell Models of Alzheimer's Disease. [Abstract]2017 Apr 11;8(4):870-882. PMID: 28285880 -
J Neurochem
Substrate determinants in the C99 juxtamembrane domains differentially affect γ-secretase cleavage specificity and modulator pharmacology. [Abstract]2013 May;125(4):610-9. PMID: 23253155 -
Reprod Domest Anim
2022 Jan;57(1):10-18. PMID: 34626138 -
Solvente y solubilidad
DMSO : 50 mg/mL (119.19 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (5.96 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (5.96 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (273 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Nakano-Ito K, et al. E2012-induced cataract and its predictive biomarkers. Toxicol Sci. 2014 Jan;137(1):249-58. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3838 mL | 11.9192 mL | 23.8385 mL | 59.5962 mL |
| 5 mM | 0.4768 mL | 2.3838 mL | 4.7677 mL | 11.9192 mL | |
| 10 mM | 0.2384 mL | 1.1919 mL | 2.3838 mL | 5.9596 mL | |
| 15 mM | 0.1589 mL | 0.7946 mL | 1.5892 mL | 3.9731 mL | |
| 20 mM | 0.1192 mL | 0.5960 mL | 1.1919 mL | 2.9798 mL | |
| 25 mM | 0.0954 mL | 0.4768 mL | 0.9535 mL | 2.3838 mL | |
| 30 mM | 0.0795 mL | 0.3973 mL | 0.7946 mL | 1.9865 mL | |
| 40 mM | 0.0596 mL | 0.2980 mL | 0.5960 mL | 1.4899 mL | |
| 50 mM | 0.0477 mL | 0.2384 mL | 0.4768 mL | 1.1919 mL | |
| 60 mM | 0.0397 mL | 0.1987 mL | 0.3973 mL | 0.9933 mL | |
| 80 mM | 0.0298 mL | 0.1490 mL | 0.2980 mL | 0.7450 mL | |
| 100 mM | 0.0238 mL | 0.1192 mL | 0.2384 mL | 0.5960 mL |
E 2012 Related Classifications
HY-10016 Related Classifications
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