Potent intermediate conductance Ca2+-activated K+ channel (KCa3.1) blocker (Kd = 60 nM). Has no effect on cytochrome p450 activity. Inhibits I-EBIO-stimulated increases in rat artery membrane potential ex vivo. Also diminishes LPS-induced cryptidin (mammalian α-defensin) release from paneth cells in vitro.
|Storage||Store at RT|
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 303.78. Batch specific molecular weights may vary from batch to batch due to solvent 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||6.58 mL||32.92 mL||65.84 mL|
|2.5 mM||1.32 mL||6.58 mL||13.17 mL|
|5 mM||0.66 mL||3.29 mL||6.58 mL|
|25 mM||0.13 mL||0.66 mL||1.32 mL|
References are publications that support the biological activity of the product.
Wulff et al (2000) Design of a potent and selective inhibitor of the intermediate-conductance Ca2+-activated K+ channel, IKCa1: a potential immunosuppressant. Proc.Natl.Acad.Sci.U.S.A. 97 8151 PMID: 10884437
Burnham et al (2006) Impaired small-conductance Ca2+-activated K+ channel-dependent EDHF responses in Type II diabetic ZDF rats. Br.J.Pharmacol. 148 434 PMID: 16682967
Ayabe et al (2002) Modulation of mouse Paneth cell alpha-defensin secretion by mIKCa1, a Ca2+-activated, intermediate conductance potassium channel. J.Biol.Chem. 277 3793 PMID: 11724775
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Keywords: TRAM 39, TRAM 39 supplier, TRAM39, potent, intermediate, conductance, calcium, Ca2+, actiavted, potassium, K+, channels, blockers, blocks, KCa3.1, IKCa1, ion, Ca2+-Activated, Potassium, Channels, 4952, Tocris Bioscience
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Product was used on BK channel.Calcium activated potassium channels were expressed by HEK 293 cells which was used for the study.It shows moderate blocking activity and the data patterns were similar throughout the study.
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.