E 2012

Name: E 2012
Brand: MedChemExpress
SKU: HY-10016
Rating: 5.0 (8 reviews)

Cat. No.: HY-10016 Purity: 97.08%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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.

For research use only. We do not sell to patients.

E 2012 Chemical Structure

CAS No. : 870843-42-8

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 110	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 110	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 100	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 150	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 1100	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Based on 8 publication(s) in Google Scholar

7 Publications Citing Use of MCE E 2012

•bioRxiv. 2024 September 13.

: 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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Biological Activity
Purity & Documentation
References
Customer Review

Description

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	0.16 μM Compound: 3, E2012	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	[PMID: 24139583]
HEK293	IC₅₀	14000 nM Compound: 1, E-2012	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	[PMID: 22098494]
HEK293	IC₅₀	2300 nM Compound: 1, E-2012	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	[PMID: 22098494]
HEK293	IC₅₀	560 nM Compound: E2012	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	[PMID: 26142947]
HEK293	IC₅₀	64 nM Compound: 2	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	[PMID: 32786237]
HEK293	IC₅₀	64 nM Compound: 1, E-2012	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	[PMID: 22098494]
HEK293	IC₅₀	64 nM Compound: 1	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	[PMID: 21195610]
HEK293	IC₅₀	85 nM Compound: E2012	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	[PMID: 26142947]

In Vitro

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.

In Vivo

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^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

419.49

Formula

C₂₅H₂₆FN₃O₂

CAS No.

870843-42-8

Appearance

Solid

Color

Light yellow to yellow

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.3838 mL	11.9192 mL	23.8385 mL
5 mM	0.4768 mL	2.3838 mL	4.7677 mL
10 mM	0.2384 mL	1.1919 mL	2.3838 mL

View the 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.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.

Protocol 1

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.
Protocol 2

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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.96 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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.

Purity & Documentation

Purity: 97.08%

Select Batch:

Data Sheet (273 KB) SDS (251 KB)

COA (246 KB) HNMR (263 KB) LCMS (101 KB)

Handling Instructions (2659 KB)

References

[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

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

Neurological Disease

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

E 2012870843-42-8E2012E-2012γ-secretaseGamma secretaseInhibitorinhibitorinhibit

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E 2012

Customer Review

E 2012 Related Antibodies

7 Publications Citing Use of MCE E 2012

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E 2012 Related Antibodies

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Complete Stock Solution Preparation Table

E 2012 Related Classifications

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