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AEP-IN-3 (compound 18) is an orally active, potent and brain penetrant asparagine endopeptidase (AEP) inhibitor, with an IC50 of 7.8 ± 0.9 nM. AEP-IN-3 can be used for Alzheimer’s Disease (AD) research.

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

AEP-IN-3 Chemical Structure

AEP-IN-3 Chemical Structure

CAS No. : 2978521-26-3

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5 mg USD 980 In-stock
10 mg USD 1650 In-stock
25 mg USD 3300 In-stock
50 mg USD 5280 In-stock
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Based on 1 publication(s) in Google Scholar

AEP-IN-3 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

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Description

AEP-IN-3 (compound 18) is an orally active, potent and brain penetrant asparagine endopeptidase (AEP) inhibitor, with an IC50 of 7.8 ± 0.9 nM. AEP-IN-3 can be used for Alzheimer’s Disease (AD) research[1].

In Vivo

AEP-IN-3 (compound 18) has a bioavailability of 83% and a T1/2[1].
AEP-IN-3 (20 mg/kg, orally, BID, for 5 days) shows significantly inhibited activity of AEP in brain in TauP301L transgenic mice[1].

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

Animal Model: Mice producing the 2N4R isoform of human Tau containing the P301L mutation in a FVB/N genetic background (3.8 months old)[1]
Dosage: 20 mg/kg
Administration: Orally, BID with an interval of 7-8 h between doses for 5 days
Result: Showed significantly inhibited activity of AEP in brain, reduced formation of the Tau N368 fragment. The effect on total Tau is not significant.
Molecular Weight

455.40

Formula

C21H21F4N3O4
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(N1C[C@H](F)C[C@H]1C(N[C@@H](CC(N)=O)C#C)=O)C2(CC2)C3=CC=C(OC(F)(F)F)C=C3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (219.59 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 2.1959 mL 10.9794 mL 21.9587 mL
5 mM 0.4392 mL 2.1959 mL 4.3917 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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Volume (start)

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C2

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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: 2.5 mg/mL (5.49 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 (5.49 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.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1959 mL 10.9794 mL 21.9587 mL 54.8968 mL
5 mM 0.4392 mL 2.1959 mL 4.3917 mL 10.9794 mL
10 mM 0.2196 mL 1.0979 mL 2.1959 mL 5.4897 mL
15 mM 0.1464 mL 0.7320 mL 1.4639 mL 3.6598 mL
20 mM 0.1098 mL 0.5490 mL 1.0979 mL 2.7448 mL
25 mM 0.0878 mL 0.4392 mL 0.8783 mL 2.1959 mL
30 mM 0.0732 mL 0.3660 mL 0.7320 mL 1.8299 mL
40 mM 0.0549 mL 0.2745 mL 0.5490 mL 1.3724 mL
50 mM 0.0439 mL 0.2196 mL 0.4392 mL 1.0979 mL
60 mM 0.0366 mL 0.1830 mL 0.3660 mL 0.9149 mL
80 mM 0.0274 mL 0.1372 mL 0.2745 mL 0.6862 mL
100 mM 0.0220 mL 0.1098 mL 0.2196 mL 0.5490 mL
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AEP-IN-3 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:

AEP-IN-32978521-26-3OthersOrally AvailableBrain PenetrantAlzheimer’s DiseaseInhibitorinhibitorinhibit

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