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High affinity, selective KCa2.2 (SK2) channel blocker (Kd = 3.8 nM). Exhibits >200-fold selectivity for KCa2.2 over KCa2.1, KCa2.3, KCa3.1, IK, Kv and Kir2.1. Increases theta-burst responses and increases LTP in rat hippocampal slices in vitro. Convulsive in vivo.
(Modifications: X = Dab, Disulfide bridges: 3-21, 8-26, 12-28, His-31 = C-terminal amide)
|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.
|Solubility||Soluble to 1 mg/ml in water|
References are publications that support the biological activity of the product.
Shakkottai et al (2001) Design and characterization of a highly selective peptide inhibitor of the small conductance calcium-activated K+ channel, SkCa2. J.Biol.Chem. 276 43145 PMID: 11527975
Kramar et al (2004) A novel mechanism for the facilitation of theta-induced long-term potentiation by brain-derived neurotrophic factor. J.Neurosci. 24 5151 PMID: 15175384
Kasumu et al (2012) Selective positive modulator of calcium-activated potassium channels exerts beneficial effects in a mouse model of spinocerebellar ataxia type 2. Chem.Biol. 19 1340 PMID: 23102227
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Keywords: Lei-Dab 7, Lei-Dab 7 supplier, Lei-Dab7, selective, potent, small, conductance, calcium, activated, potassium, channels, K+, Ca2+, inhibitors, inhibits, KCa2.2, SK2, blockers, Ca2+-Activated, Potassium, Channels, 5571, Tocris Bioscience
1 Citation for Lei-Dab 7
Citations are publications that use Tocris products. Selected citations for Lei-Dab 7 include:
Sargin et al (2016) Chronic social isolation reduces 5-HT neuronal activity via upregulated SK3 calcium-activated potassium channels Elife 5 e21416 PMID: 27874831
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Reviews for Lei-Dab 7
Average Rating: 4 (Based on 1 Review.)
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The product is a great high affinity calcium-activated potassium channel activator which shows great variation in concentration dependent channel opening. The product works ideally on labs and the data produced can be easily reproduced. One con of the product will be that it has very little safety data accompanying it.
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.