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.
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- CAS No.: 15437-29-3
- 화학식: C20H15Cl2NO3
- 분자량:388.24
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
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CLC-2 14 (rat) nM (IC50) |
CLC-2 17 (human) nM (IC50) |
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.
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
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CAS No. 15437-29-3
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분자량 388.24
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화학식 C20H15Cl2NO3
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SMILES
O=C(C1=C(NC2=C(Cl)C(OCC3=CC=CC=C3)=CC=C2Cl)C=CC=C1)O
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)