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Selective Na+/Ca2+-exchange (NCX) inhibitor; displays some selectivity for NCX1. IC50 values are 2.9, 16 and 8.6 μM for inhibition of intracellular Na+-dependent 45Ca2+ uptake by cells expressing NCX1, NCX2 and NCX3 respectively. Has some affinity for mACh receptors (IC50 = 18 μM) but minimal activity against NCKX2 and various receptors and ion channels (IC50 > 30 μM). Preferentially blocks Ca2+ influx mode and is more selective for NCX isoforms than KB-R7943 (Cat. No. 1244). Anti-ischemic; potently protects against hypoxia-induced renal tubular cell damage (IC50 = 0.63 μM).
|Storage||Desiccate at +4°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 402.16. 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||2.49 mL||12.43 mL||24.87 mL|
|5 mM||0.5 mL||2.49 mL||4.97 mL|
|10 mM||0.25 mL||1.24 mL||2.49 mL|
|50 mM||0.05 mL||0.25 mL||0.5 mL|
References are publications that support the biological activity of the product.
Iwamoto et al (2004) The exchanger inhibitory peptide region-dependent inhibition of Na+/Ca2+ exchange by SN-6 [2-[4-(4-nitrobenzyloxy)benzyl]thiazolidine-4-carboxylic acid ethyl ester], a novel benzyloxyphenyl derivative. Mol.Pharmacol. 66 45 PMID: 15213295
Iwamoto (2004) Forefront of Na+/Ca2+ exchanger studies: molecular pharmacology of N+/Ca2+ exchange inhibitors. J.Pharmacol.Sci. 96 27 PMID: 15359084
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Keywords: SN-6, SN-6 supplier, Selective, Na+/Ca2+, exchange, inhibitors, inhibits, reverse, mode, Sodium, Calcium, Exchanger, Ion, Transporters, Pumps, Ca2+, Signaling, Signalling, NCX1, 2184, Tocris Bioscience
8 Citations for SN-6
Citations are publications that use Tocris products. Selected citations for SN-6 include:
Bastioli et al (2019) Selective inhibition of mitochondrial sodium-calcium exchanger protects striatal neurons from α-synuclein plus rotenone induced toxicity. Cell Death Dis 10 80 PMID: 30692508
Wang et al (2012) Astrocytes modulate neural network activity by Ca2+-dependent uptake of extracellular K+. Cell Cycle 5 ra26 PMID: 22472648
Wang et al (2015) Conditional knockout of smooth muscle sodium calcium exchanger type-1 lowers blood pressure and attenuates Angiotensin II-salt hypertension. Sci Signal 3 PMID: 25626872
Fu and Pol (2010) Kisspeptin directly excites anorexigenic proopiomelanocortin neurons but inhibits orexigenic neuropeptide Y cells by an indirect synaptic mechanism. J Neurosci 30 10205 PMID: 20668204
Piccirillo (2018) Glutamate as a potential "survival factor" in an in vitro model of neuronal hypoxia/reoxygenationinjury: leading role of the Na+/Ca2+ exchanger. Cell Death Dis 9 731 PMID: 29955038
Pezier et al (2009) The Na+/Ca2+ exchanger inhibitor, KB-R7943, blocks a nonselective cation channel implicated in chemosensory transduction. J Neurophysiol 101 1151 PMID: 19118110
Ciapa and Philippe (2013) Intracellular and extracellular pH and Ca are bound to control mitosis in the early sea urchin embryo via ERK and MPF activities. PLoS One 8 e66113 PMID: 23785474
Barrientos et al (2009) The Na+/Ca2+ exchange inhibitor 2-(2-(4-(4-nitrobenzyloxy)phenyl)ethyl)isothiourea methanesulfonate (KB-R7943) also blocks ryanodine receptors type 1 (RyR1) and type 2 (RyR2) channels. Mol Pharmacol 76 560 PMID: 19509218
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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.