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Cat. No.: HY-182571

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AK-42

AK-42 is a selective CLC-2 chloride channel inhibitor with human IC₅₀ of 17 nM and rat IC₅₀ of 14 nM. AK-42 binds to an extracellular vestibule above the channel pore, inhibits CLC-2 currents acutely and reversibly, including with auxiliary subunit GlialCAM coexpression. AK-42 acts as a selective tool compound for acute CLC-2 function modulation to probe CLC-2 neurophysiology. AK-42 can be used for the research of leukodystrophy and idiopathic generalized epilepsies.

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

CAS No.: 15437-29-3
Formula: C₂₀H₁₅Cl₂NO₃
Molecular Weight:388.24

Storage:

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

AK-42 Chemical Structure

CAS No.: 15437-29-3

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Fluorescent Dye

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

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

Biological Activity

Description

IC₅₀ & Target^[1]

CLC-2

14 (rat) nM (IC₅₀)

CLC-2

17 (human) nM (IC₅₀)

In Vitro

AK-42 (5 min) potently inhibits human CLC-2 chloride currents stably expressed in CHO cells with an IC₅₀ of 17 nM, and displays >1000-fold selectivity over CLC-1 with minimal off-target activity against other CNS membrane proteins and anion channels^[1].
AK-42 potently and reversibly inhibits rat CLC-2 chloride currents transiently expressed in CHO cells with an IC₅₀ of 14 nM, with comparable efficacy against CLC-2 coexpressed with GlialCAM, and its binding is dependent on specific extracellular channel residues including K210 and Q399^[1].

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

Application

1. This compound can be used as a tracer
2. This compound can be used as an internal standard for quantitative analysis by NMR, GC-MS, or LC-MS.

Chemical Information

CAS No. 15437-29-3
Molecular Weight 388.24
Formula C₂₀H₁₅Cl₂NO₃
SMILES

O=C(C1=C(NC2=C(Cl)C(OCC3=CC=CC=C3)=CC=C2Cl)C=CC=C1)O
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]. Koster AK, et al. Development and validation of a potent and specific inhibitor for the CLC-2 chloride channel. Proc Natl Acad Sci U S A. 2020;117(51):32711-32721. [Content Brief]

Calculators

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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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