An activator of Kv7.2/Kv7.3 subunit-containing channels
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ICA 27243

Item No. 40827

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-(6-chloro-3-pyridinyl)-3,4-difluoro-benzamide
CAS Number
325457-89-4
Synonyms
  • ICA027243
Molecular Formula
C12H7ClF2N2O
Formula Weight
268.7
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble: ≥10 mg/mlEthanol: Sparingly Soluble: 1-10 mg/ml
SMILES
O=C(C1=CC=C(C(F)=C1)F)NC2=CN=C(C=C2)Cl
InChi Code
InChI=1S/C12H7ClF2N2O/c13-11-4-2-8(6-16-11)17-12(18)7-1-3-9(14)10(15)5-7/h1-6H,(H,17,18)
InChi Key
GDGUOCFTHNGPBK-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    5 mg

    $107

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    10 mg

    $203

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    50 mg

    $854

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    100 mg

    $1,494

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    Product Description

    ICA 27243 is an activator of heteromeric voltage-gated potassium channels containing Kv7.2 and Kv7.3 subunits (Kv7.2/Kv7.3).1 It enhances rubidium efflux in an agonist-induced rubidium efflux assay using CHO cells expressing Kv7.2/Kv7.3 channels (EC50 = 0.38 µM). ICA 27243 is selective for heteromeric Kv7.2/Kv7.3 channels over homomeric Kv7.4 channels (EC50 = 7.1 µM) and is 100-300-fold selective for Kv7.2/Kv7.3 over Kv7.3/Kv7.5 channels.2 It is also selective for Kv7.2/Kv7.3 channels over a panel of neurotransmitter receptors and voltage-gated sodium channel Nav1.2 at 10 µM, as well as GABAA receptors and high voltage-activated calcium channels at 30 µM. ICA 27243 protects against maximal electroshock-induced seizures in a rat model of epilepsy (ED50 = 1.5 mg/kg).1 It also prevents hyperactivity induced by amphetamine and chlordiazepoxide, but not by amphetamine alone, without affecting basal locomotor activity in a mouse model of manic-like hyperactivity when administered at a dose of 10 mg/kg.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Amato, G., Roeloffs, R., Rigdon, G.C., et al. N-Pyridyl and pyrimidine benzamides as KCNQ2/Q3 potassium channel openers for the treatment of epilepsy. ACS Med. Chem. Lett. 2(6), 481-484 (2011).

    2. Wickenden, A.D., Krajewski, J.L., London, B., et al. N-(6-chloro-pyridin-3-yl)-3,4-difluoro-benzamide (ICA-27243): A novel, selective KCNQ2/Q3 potassium channel activator. Mol. Pharmacol. 73(3), 977-986 (2008).

    3. Redrobe, J.P., and Nielsen, A.N. Effects of neuronal Kv7 potassium channel activators on hyperactivity in a rodent model of mania. Behav. Brain Res. 198(2), 481-485 (2009).