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Positive allosteric modulator of KCa3.1 (intermediate-conductance Ca2+-activated potassium) channels (EC50 = 109 nM). Displays 40-fold selectivity for KCa3.1 over KCa2.3, and 200 to 400-fold selectivity over KV and NaV channels. Potentiates bradykinin-induced vasodilation ex vivo. Lowers mean arterial blood pressure in normotensive and hypertensive mice.
|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 198.23. 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||5.04 mL||25.22 mL||50.45 mL|
|5 mM||1.01 mL||5.04 mL||10.09 mL|
|10 mM||0.5 mL||2.52 mL||5.04 mL|
|50 mM||0.1 mL||0.5 mL||1.01 mL|
References are publications that support the biological activity of the product.
Coleman et al (2014) New positive Ca2+-activated K+ channel gating modulators with selectivity for KCa3.1. Mol.Pharmacol. 86 342 PMID: 24958817
Oliván-Viguera et al (2016) Vascular reactivity profile of novel KCa 3.1-selective positive-gating modulators in the coronary vascular bed. Basic Clin.Pharmacol.Toxicol. 119 184 PMID: 26821335
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Keywords: SKA 121, SKA 121 supplier, SKA121, calcium, sensitive, activated, potassium, channel, positive, allosteric, modulators, modulates, kca3.1, intermediate, conductance, SK4, IK, blood, pressure, vasodilation, Ca2+-Activated, Potassium, Channels, 6398, Tocris Bioscience
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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.