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Selective Kv7.1 (KCNQ1) potassium channel activator (EC50 = 260 nM). Exhibits >100-fold selectivity versus KCNQ2, KCNQ4 and hERG potassium channels. Augments IKs current of cultured human cardiomyocytes and shortens action potential duration.
|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 471.59. 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||2.12 mL||10.6 mL||21.2 mL|
|5 mM||0.42 mL||2.12 mL||4.24 mL|
|10 mM||0.21 mL||1.06 mL||2.12 mL|
|50 mM||0.04 mL||0.21 mL||0.42 mL|
References are publications that support the biological activity of the product.
Mattmann et al (2012) Identification of (R)-N-(4-(4-methoxyphenyl)thiazol-2-yl)-1-tosylpiperidine-2-carboxamide, ML277, as a novel, potent and selective Kv7.1 (KCNQ1) potassium channel activator. Bioorg.Med.Chem.Lett. 22 5936 PMID: 22910039
Yu et al (2013) Dynamic subunit stoichiometry confers a progressive continuum of pharmacological sensitivity by KCNQ potassium channels. Proc.Natl.Acad.Sci.U.S.A. 110 8732 PMID: 23650380
If you know of a relevant reference for ML 277, please let us know.
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Citations for ML 277
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Reviews for ML 277
Average Rating: 5 (Based on 1 Review.)
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ML 277 is being used on our lab for its selective channel activation properties. It shows great Kv channel opening properties. Have been used in published papers and the data produced are consistent.
Dissolve in DMSO. For sterile conditions, use sterile DMSO.
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.