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ICA 121431 is a potent and selective inhibitor of human NaV1.3 and NaV1.1 channels (IC50 values are 13 and 23 nM respectively). Exhibits up to 1,000 fold selectivity against other TTX-sensitive or resistant sodium channels (IC50 values are >10 μM for human NaV1.5 and NaV1.8 channels). Interacts with an inhibitory interaction site distinct from those bound by TTX and local anesthetic-like modulators.
ICA 121431 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
|Storage||Store at +4°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
The following data is based on the product molecular weight 449.55. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.22 mL||11.12 mL||22.24 mL|
|5 mM||0.44 mL||2.22 mL||4.45 mL|
|10 mM||0.22 mL||1.11 mL||2.22 mL|
|50 mM||0.04 mL||0.22 mL||0.44 mL|
References are publications that support the biological activity of the product.
McCormack et al (2013) Voltage sensor interaction site for selective small molecule inhibitors of voltage-gated sodium channels. Proc.Natl.Acad.Sci. 110 2724 PMID: 23818614
If you know of a relevant reference for ICA 121431, please let us know.
Keywords: ICA 121431, ICA 121431 supplier, Selective, NaV, blockers, Sodium, Channels, voltage-gated, voltage-dependent, Na+, ICA121431, Voltage-gated, 5066, Tocris Bioscience
Citations are publications that use Tocris products. Selected citations for ICA 121431 include:
Kocmalova et al (2017) Control of Neurotransmission by NaV1.7 in Human, Guinea Pig, and Mouse Airway Parasympathetic Nerves. J Pharmacol Exp Ther 361 172 PMID: 28138042
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Epilepsy is a brain disease that affects 60 million people globally. More than 20 anti-seizure drugs are currently available, but these do not address the underlying causes of the condition. This poster summarizes current knowledge about the development of the condition and highlights some approaches that have disease-modifying effects in proof-of-concept studies.