An Nav1.1 activator
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AA43279

Item No. 40428

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3-amino-5-(4-methoxyphenyl)-2-thiophenecarboxamide
CAS Number
354812-16-1
Molecular Formula
C12H12N2O2S
Formula Weight
248.3
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
Acetonitrile: SolubleDMSO: Soluble
SMILES
O=C(C1=C(N)C=C(C2=CC=C(C=C2)OC)S1)N
InChi Code
InChI=1S/C12H12N2O2S/c1-16-8-4-2-7(3-5-8)10-6-9(13)11(17-10)12(14)15/h2-6H,13H2,1H3,(H2,14,15)
InChi Key
OEUITKOCUWEFOB-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    5 mg

    $54

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    10 mg

    $97

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    25 mg

    $216

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    50 mg

    $378

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    Product Description

    AA43279 is an activator of voltage-gated sodium channel 1.1 (Nav1.1; EC50 = 9.5 µM in a patch-clamp assay using HEK293 cells expressing the human channel).1 It is selective for Nav1.1 over Nav1.4 and Nav1.7 at 30 µM but also activates Nav1.2, Nav1.5, and Nav1.6 (EC50s = 22.8, 14.4, and 11.6 µM, respectively). AA43279 also inhibits IκB kinase β (IKKβ; IC50 = 2.9 µM).2 It increases the seizure threshold in the maximal electroshock seizure threshold (MEST) test in mice when administered at a dose of 300 mg/kg.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Frederiksen, K., Lu, D., Yang, J., et al. A small molecule activator of Nav 1.1 channels increases fast-spiking interneuron excitability and GABAergic transmission in vitro and has anti-convulsive effects in vivo. Eur. J. Neurosci. 46(3), 1887-1896 (2017).

    2. Morwick, T., Berry, A., Brickwood, J., et al. Evolution of the thienopyridine class of inhibitors of IκB kinase-β: part I: Hit-to-lead strategies. J. Med. Chem. 49(10), 2898-2908 (2006).