2. Neuronal Signaling
  3. Beta-secretase
  4. Elenbecestat

Elenbecestat  (Synonyms: E2609)

Cat. No.: HY-109055 Purity: 99.94%
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Elenbecestat (E2609) is a potent, orally bioavailable and CNS-penetrant BACE-1 inhibitor. Elenbecestat has the potential for Alzheimer's disease (AD) research.

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

Elenbecestat Chemical Structure

Elenbecestat Chemical Structure

CAS No. : 1388651-30-6

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Solid + Solvent
10 mM * 1 mL in DMSO
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 USD 209 In-stock
Solution
10 mM * 1 mL in DMSO USD 209 In-stock
Solid
5 mg USD 190 In-stock
10 mg USD 320 In-stock
25 mg USD 660 In-stock
50 mg USD 1100 In-stock
100 mg USD 1700 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Elenbecestat Related Antibodies

Top Publications Citing Use of Products

View All Beta-secretase Isoform Specific Products:

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BACE1 BACE2

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Elenbecestat (E2609) is a potent, orally bioavailable and CNS-penetrant BACE-1 inhibitor. Elenbecestat has the potential for Alzheimer's disease (AD) research[1][2].

IC50 & Target

BACE-1[1]
In Vitro

Elenbecestat (E2609) is a potent BACE1 inhibitor with an IC50 of ~7 nmol/L in cell-based assay[2].
Elenbecestat has been shown to reduce Ab production in the plasma, brain, and cerebrospinal fluid (CSF) of rodents[2].

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

Elenbecestat Related Antibodies
In Vivo

Elenbecestat (E2609; 0.3-30 mg/kg; p.o.) potently inhibits Ab1-40 and Ab1-42 production in the plasma and CSF of non-human primates[2].
Elenbecestat displays the plasma half-life of 12-16 hours after once daily dosing[1].

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

Animal Model: Cynomolgus monkeys (Pharmacokinetic analysis)[2]
Dosage: 0.3 mg/kg; 1 mg/kg; 3 mg/kg; 30 mg/kg
Administration: Oral administration
Result: Potently inhibits Ab1-40 and Ab1-42 production in the plasma and CSF.
Clinical Trial
Molecular Weight

437.44

Formula

C19H18F3N5O2S
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

FC1=CC=C(NC(C2=NC=C(C(F)F)N=C2)=O)C=C1[C@@]3(N=C(N)SC4)[C@@]4([H])[C@@H](C)OC3
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 : 100 mg/mL (228.60 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 2.2860 mL 11.4301 mL 22.8603 mL
5 mM 0.4572 mL 2.2860 mL 4.5721 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)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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: ≥ 2.08 mg/mL (4.75 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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% Corn Oil

    Solubility: ≥ 2.08 mg/mL (4.75 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 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 (20.8 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)

g

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
References

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 2.2860 mL 11.4301 mL 22.8603 mL 57.1507 mL
5 mM 0.4572 mL 2.2860 mL 4.5721 mL 11.4301 mL
10 mM 0.2286 mL 1.1430 mL 2.2860 mL 5.7151 mL
15 mM 0.1524 mL 0.7620 mL 1.5240 mL 3.8100 mL
20 mM 0.1143 mL 0.5715 mL 1.1430 mL 2.8575 mL
25 mM 0.0914 mL 0.4572 mL 0.9144 mL 2.2860 mL
30 mM 0.0762 mL 0.3810 mL 0.7620 mL 1.9050 mL
40 mM 0.0572 mL 0.2858 mL 0.5715 mL 1.4288 mL
50 mM 0.0457 mL 0.2286 mL 0.4572 mL 1.1430 mL
60 mM 0.0381 mL 0.1905 mL 0.3810 mL 0.9525 mL
80 mM 0.0286 mL 0.1429 mL 0.2858 mL 0.7144 mL
100 mM 0.0229 mL 0.1143 mL 0.2286 mL 0.5715 mL
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Elenbecestat Related Classifications

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:

Elenbecestat1388651-30-6E2609E 2609E-2609Beta-secretaseBACEβ-SecretaseBACE-1Alzheimer's diseaseADInhibitorinhibitorinhibit

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