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

Atabecestat  (Synonyms: JNJ-54861911)

Cat. No.: HY-109052 Purity: 99.77%
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Atabecestat (JNJ-54861911) is a potent brain-penetrant and orally active β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor, achieves robust and high CSF Aβ reduction. Atabecestat s tolerated and displays a sustained pharmacokinetic (PK) and pharmacodynamic (PD) characteristics. Atabecestat has the potential for Alzheimer's Disease treatment.

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

Atabecestat Chemical Structure

Atabecestat Chemical Structure

CAS No. : 1200493-78-2

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 440 In-stock
Solution
10 mM * 1 mL in DMSO USD 440 In-stock
Solid
5 mg USD 400 In-stock
10 mg USD 640 In-stock
25 mg USD 1280 In-stock
50 mg   Get quote  
100 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

Atabecestat (JNJ-54861911) is a potent brain-penetrant and orally active β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor, achieves robust and high CSF Aβ reduction. Atabecestat s tolerated and displays a sustained pharmacokinetic (PK) and pharmacodynamic (PD) characteristics. Atabecestat has the potential for Alzheimer's Disease treatment[1].

IC50 & Target

BACE1

 

In Vivo

Atabecestat (100 and 300 mg/kg; p.o. once daily for 3 days) reduces the human Aβ levels in mice[2].
Atabecestat (300 mg/kg; p.o. once) inhibits the exacerbation of vascular abnormalities in APPPS1 mice with 3D6 treatment[2].

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

Animal Model: 5-week-old APPPS1 mice[2]
Dosage: 100 and 300 mg/kg
Administration: Oral gavage; 100 and 300 mg/kg; once daily for 3 days
Result: Reduced the level of human Aβ1-40 and Aβ1-42 levels in the brain of APPPS1 mice at a dose of 300 mg/kg and resulted in less reduction of human Aβ levels at 24 h with a dose of 100 mg/kg.
Clinical Trial
Molecular Weight

367.40

Formula

C18H14FN5OS
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=NC=C(C#N)C=C1)NC2=CC=C(F)C([C@@]3(C)N=C(N)SC=C3)=C2
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 : 250 mg/mL (680.46 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 2.7218 mL 13.6091 mL 27.2183 mL
5 mM 0.5444 mL 2.7218 mL 5.4437 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.

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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

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Volume (start)

V1

=
Concentration (final)

C2

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Volume (final)

V2

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.
Calculation results:
Working solution concentration: mg/mL
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 2.7218 mL 13.6091 mL 27.2183 mL 68.0457 mL
5 mM 0.5444 mL 2.7218 mL 5.4437 mL 13.6091 mL
10 mM 0.2722 mL 1.3609 mL 2.7218 mL 6.8046 mL
15 mM 0.1815 mL 0.9073 mL 1.8146 mL 4.5364 mL
20 mM 0.1361 mL 0.6805 mL 1.3609 mL 3.4023 mL
25 mM 0.1089 mL 0.5444 mL 1.0887 mL 2.7218 mL
30 mM 0.0907 mL 0.4536 mL 0.9073 mL 2.2682 mL
40 mM 0.0680 mL 0.3402 mL 0.6805 mL 1.7011 mL
50 mM 0.0544 mL 0.2722 mL 0.5444 mL 1.3609 mL
60 mM 0.0454 mL 0.2268 mL 0.4536 mL 1.1341 mL
80 mM 0.0340 mL 0.1701 mL 0.3402 mL 0.8506 mL
100 mM 0.0272 mL 0.1361 mL 0.2722 mL 0.6805 mL
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Atabecestat 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:

Atabecestat1200493-78-2JNJ-54861911JNJ54861911JNJ 54861911Beta-secretaseBACEβ-SecretaseBACE1AβCSFAlzheimerDiseaseInhibitorinhibitorinhibit

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