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Cat. No.: HY-100182A

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BACE1-IN-1 hydrochloride

BACE1-IN-1 hydrochloride is an orally active, blood-brain barrier penetrant dual-target inhibitor of BACE1/2, with IC₅₀ values of 23 nM and 24 nM against human BACE1 and BACE2, respectively. BACE1-IN-1 hydrochloride reduces cerebral Aβ40 levels in mice. BACE1-IN-1 hydrochloride can be used in studies related to Alzheimer's disease and type 2 diabetes.

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

CAS No.: 1310349-35-9
Formula: C₁₈H₁₅ClF₃N₅O₂
Molecular Weight:425.79

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

BACE1-IN-1 hydrochloride Chemical Structure

CAS No.: 1310349-35-9

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
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Biological Activity

Description

IC₅₀ & Target^[1]^[2]

BACE1

23 nM (IC₅₀)

BACE2

24 nM (IC₅₀)

All Beta-secretase Isoforms :

BACE1
BACE2

In Vitro

BACE1-IN-1 hydrochloride inhibits Aβ40 production in HEK293 cells with an IC₅₀ of 0.018-0.021 μM; it exhibits an enzymatic IC₅₀ of 0.023 μM against hBACE1, an enzymatic IC₅₀ of 0.024 μM against hBACE2, and an IC₅₀ of 0.074 μM for inhibiting BACE2 in INS-TMEM27 cells^[1]^[2].

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

In Vivo

BACE1-IN-1 (10-30 mg/kg; p.o.; single administration) hydrochloride reduces cerebral Aβ40 levels in wild-type mice^[2].

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

Animal Model:

Female C57Bl/6J wild-type mice^[2]
Dosage:

10 mg/kg, 30 mg/kg
Administration:

Oral gavage (p.o.)
Result:

Animals were sacrificed 4 hours after administration, and brain tissue was taken to detect Aβ40 levels.
Brain Aβ40 decreased by 78% in the 10 mg/kg group.
Brain Aβ40 decreased by 84% in the 30 mg/kg group.

Chemical Information

CAS No. 1310349-35-9
Molecular Weight 425.79
Formula C₁₈H₁₅ClF₃N₅O₂
SMILES

C[C@]1(C(F)(COC(N)=N1)F)C2=CC(NC(C3=CC=C(C=N3)C#N)=O)=CC=C2F.Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Banner D, et al. Preparation of 2-amino-5, 5-difluoro-5, 6-dihydro-4H-oxazine derivatives as BACE1 and/or BACE2 inhibitors[J]. International Patent WO2011069934.(c) Shishido, Y, 2011: 7193-7205.

[2]. Hilpert H, et al. β-Secretase (BACE1) inhibitors with high in vivo efficacy suitable for clinical evaluation in Alzheimer's disease. J Med Chem. 2013 May 23;56(10):3980-95. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References

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BACE1-IN-1 hydrochloride

All Beta-secretase Isoforms