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^[1].

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.

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.

388.24

C₂₀H₁₅Cl₂NO₃

15437-29-3

O=C(C1=C(NC2=C(Cl)C(OCC3=CC=CC=C3)=CC=C2Cl)C=CC=C1)O

Room temperature in continental US; may vary elsewhere.

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

• [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.