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KC 12291 hydrochloride
Orally active atypical voltage-gated sodium channel blocker. Inhibits sustained sodium currents (INaL) and prevents diastolic contracture in isolated atria in vitro (IC50 values are 9.6 and 0.55 - 0.79 μM respectively). Displays anti-ischemic, bradycardic and cardioprotective activity in vivo.
|Storage||Desiccate 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|
Preparing Stock Solutions
The following data is based on the product molecular weight 449.99. 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|
|0.5 mM||4.44 mL||22.22 mL||44.45 mL|
|2.5 mM||0.89 mL||4.44 mL||8.89 mL|
|5 mM||0.44 mL||2.22 mL||4.44 mL|
|25 mM||0.09 mL||0.44 mL||0.89 mL|
References are publications that support the biological activity of the product.
Tamareille et al (2002) Anti-ischemic compound KC 12291 prevents diastolic contracture in isolated atria by blockade of voltage-gated sodium channels. J.Cardiovasc.Pharmacol. 40 346 PMID: 12198320
John et al (2004) KC 12291: an atypical sodium channel blocker with myocardial antiischemic properties. Cardiovasc.Drug Rev. 22 17 PMID: 14978516
Letienne et al (2006) Pharmacological characterisation of sodium channels in sinoatrial node pacemaking in the rat heart. Eur.J.Pharmacol. 530 243 PMID: 16368090
Decking et al (1998) Cardioprotective actions of KC 12291. Naunyn-Schmied.Arch.Pharmacol. 358 547
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Literature in this Area
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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.