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Kv11.1 (hERG) channel blocker, blocks rapidly activating and slowly activating components of delayed rectifier K+ currents (IC50 of 0.4 mM and 3 mM, respectively). Also inhibits Na+/Ca2+ exchanger in vitro. Shows inhibition of Na+ currents, L-type Ca2+ currents and other K+ currents at high concentrations.
|Storage||Store at -20°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 530.88. 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|
|0.01 mM||188.37 mL||941.83 mL||1883.66 mL|
|0.05 mM||37.67 mL||188.37 mL||376.73 mL|
|0.1 mM||18.84 mL||94.18 mL||188.37 mL|
|0.5 mM||3.77 mL||18.84 mL||37.67 mL|
References are publications that support the biological activity of the product.
Watanabe and Kimura (2010) Inhibitory Effect of Azimilide on Na+/Ca2+ Exchange Current in Guinae-Pig Cardiac Myocytes. J.Pharmacol.Sci. 114 111 PMID: 20710119
Busch et al (1998) Blockade of HERG channels by the class III antiarrhythmic Azimilide: mode of action. Br.J.Pharmacol. 123 23 PMID: 9484850
Busch et al (1995) Blockade of Human IsK channels expression in Xenopus oocytes by the novel class III antiarrhythmic NE-10064. Eur.J.Pharmacol. 264 33 PMID: 7828640
Fermini et al (1995) Use-dependent effects of the class III antiarrhythmic agent NE-10064 (azimilide) on cardiac repolarisation: block of delayed rectifier potassium and L-type calcium currents. J.Cardiovasc.Pharmacol. 26 259 PMID: 7475051
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Keywords: Azimilide dihydrochloride, Azimilide dihydrochloride supplier, potassium, channel, blockers, Kv11.1, hERG, blocks, Voltage-Gated, Potassium, Channels, Na+/Ca2+, Exchanger, 6318, Tocris Bioscience
Citations for Azimilide dihydrochloride
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Azimilide was used to study Kv11.1 channel blocking properties. Kv11.1 channels were being studied to understand the voltage gating mechanism and how the activation and blocking of the channel is different than other Kv channels.
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.
Peripheral sensitization is the reduction in the threshold of excitability of sensory neurons that results in an augmented response to a given external stimulus. This poster outlines the excitatory and inhibitory signaling pathways involved in modulation of peripheral sensitization. The role of ion channels, GPCRs, neurotrophins, and cytokines in sensory neurons are also described.