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company name :
Tocris Bioscience
product type :
chemical
product name :
1244/10
catalog :
1244/10
quantity :
10 mg (also 50 mg)
price :
232 USD
more info or order :
citations: 44
Reference
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Fortalezas S, Marques da Silva D, Gutierrez Merino C. Methyl-β-Cyclodextrin Impairs the Phosphorylation of the β₂ Subunit of L-Type Calcium Channels and Cytosolic Calcium Homeostasis in Mature Cerebellar Granule Neurons. Int J Mol Sci. 2018;19: pubmed publisher
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Hernandez Ojeda M, Ureña Guerrero M, Gutierrez Barajas P, Cardenas Castillo J, Camins A, Beas Zarate C. KB-R7943 reduces 4-aminopyridine-induced epileptiform activity in adult rats after neuronal damage induced by neonatal monosodium glutamate treatment. J Biomed Sci. 2017;24:27 pubmed publisher
Agarwal A, Wu P, Hughes E, Fukaya M, Tischfield M, Langseth A, et al. Transient Opening of the Mitochondrial Permeability Transition Pore Induces Microdomain Calcium Transients in Astrocyte Processes. Neuron. 2017;93:587-605.e7 pubmed publisher
O Donnell J, Jackson J, Robinson M. Transient Oxygen/Glucose Deprivation Causes a Delayed Loss of Mitochondria and Increases Spontaneous Calcium Signaling in Astrocytic Processes. J Neurosci. 2016;36:7109-27 pubmed publisher
Sabourin J, Bartoli F, Antigny F, Gomez A, Benitah J. Transient Receptor Potential Canonical (TRPC)/Orai1-dependent Store-operated Ca2+ Channels: NEW TARGETS OF ALDOSTERONE IN CARDIOMYOCYTES. J Biol Chem. 2016;291:13394-409 pubmed publisher
Virsolvy A, Farah C, Pertuit N, Kong L, Lacampagne A, Reboul C, et al. Antagonism of Nav channels and α1-adrenergic receptors contributes to vascular smooth muscle effects of ranolazine. Sci Rep. 2015;5:17969 pubmed publisher
Vinberg F, Wang T, Molday R, Chen J, Kefalov V. A new mouse model for stationary night blindness with mutant Slc24a1 explains the pathophysiology of the associated human disease. Hum Mol Genet. 2015;24:5915-29 pubmed publisher
Wang Y, Chen Y, Cheng R, Huang R. Role of Na⁺/Ca²⁺ exchanger in Ca²⁺ homeostasis in rat suprachiasmatic nucleus neurons. J Neurophysiol. 2015;113:2114-26 pubmed publisher
Bobkov Y, Corey E, Ache B. An inhibitor of Na(+)/Ca(2+) exchange blocks activation of insect olfactory receptors. Biochem Biophys Res Commun. 2014;450:1104-9 pubmed publisher
Drumm B, Sergeant G, Hollywood M, Thornbury K, Matsuda T, Baba A, et al. The effect of high [K(+)]o on spontaneous Ca(2+) waves in freshly isolated interstitial cells of Cajal from the rabbit urethra. Physiol Rep. 2014;2:e00203 pubmed publisher
Cuozzo F, Raciti M, Bertelli L, Parente R, Di Renzo L. Pro-death and pro-survival properties of ouabain in U937 lymphoma derived cells. J Exp Clin Cancer Res. 2012;31:95 pubmed publisher
Yamamura A, Guo Q, Yamamura H, Zimnicka A, Pohl N, Smith K, et al. Enhanced Ca(2+)-sensing receptor function in idiopathic pulmonary arterial hypertension. Circ Res. 2012;111:469-81 pubmed publisher
Clerc P, Polster B. Investigation of mitochondrial dysfunction by sequential microplate-based respiration measurements from intact and permeabilized neurons. PLoS ONE. 2012;7:e34465 pubmed publisher
Fox J, Sakamuru S, Huang R, Teneva N, Simmons S, Xia M, et al. High-throughput genotoxicity assay identifies antioxidants as inducers of DNA damage response and cell death. Proc Natl Acad Sci U S A. 2012;109:5423-8 pubmed publisher
Pandit M, Strait K, Matsuda T, Kohan D. Na delivery and ENaC mediate flow regulation of collecting duct endothelin-1 production. Am J Physiol Renal Physiol. 2012;302:F1325-30 pubmed publisher
Chouhan A, Ivannikov M, Lu Z, Sugimori M, Llinas R, MacLeod G. Cytosolic calcium coordinates mitochondrial energy metabolism with presynaptic activity. J Neurosci. 2012;32:1233-43 pubmed publisher
Yoshizumi M, Eisenach J, Hayashida K. Riluzole and gabapentinoids activate glutamate transporters to facilitate glutamate-induced glutamate release from cultured astrocytes. Eur J Pharmacol. 2012;677:87-92 pubmed publisher
Cheng H, Zhang Y, Du C, Dempsey C, Hancox J. High potency inhibition of hERG potassium channels by the sodium-calcium exchange inhibitor KB-R7943. Br J Pharmacol. 2012;165:2260-73 pubmed publisher
Pan W, Borovac J, Spicer Z, Hoenderop J, Bindels R, Shull G, et al. The epithelial sodium/proton exchanger, NHE3, is necessary for renal and intestinal calcium (re)absorption. Am J Physiol Renal Physiol. 2012;302:F943-56 pubmed publisher
Roberts D, Matsuda T, Bose R. Molecular and functional characterization of the human platelet Na(+) /Ca(2+) exchangers. Br J Pharmacol. 2012;165:922-36 pubmed publisher
Poteser M, Schleifer H, Lichtenegger M, Schernthaner M, Stockner T, Kappe C, et al. PKC-dependent coupling of calcium permeation through transient receptor potential canonical 3 (TRPC3) to calcineurin signaling in HL-1 myocytes. Proc Natl Acad Sci U S A. 2011;108:10556-61 pubmed publisher
Xu K, Zhu W, Chen L, deFilippi C, Zhang J, Xiao R. Mechanistic distinction between activation and inhibition of (Na(+)+K(+))-ATPase-mediated Ca2+ influx in cardiomyocytes. Biochem Biophys Res Commun. 2011;406:200-3 pubmed publisher
Cheng H, Smith G, Hancox J, Orchard C. Inhibition of spontaneous activity of rabbit atrioventricular node cells by KB-R7943 and inhibitors of sarcoplasmic reticulum Ca(2+) ATPase. Cell Calcium. 2011;49:56-65 pubmed publisher
Hamming K, Soliman D, Webster N, Searle G, Matemisz L, Liknes D, et al. Inhibition of beta-cell sodium-calcium exchange enhances glucose-dependent elevations in cytoplasmic calcium and insulin secretion. Diabetes. 2010;59:1686-93 pubmed publisher
Kim C, Majdi M, Xia P, Wei K, Talantova M, Spiering S, et al. Non-cardiomyocytes influence the electrophysiological maturation of human embryonic stem cell-derived cardiomyocytes during differentiation. Stem Cells Dev. 2010;19:783-95 pubmed publisher
Barrientos G, Bose D, Feng W, Padilla I, Pessah I. 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. 2009;76:560-8 pubmed publisher
Chao D, Balboni G, Lazarus L, Salvadori S, Xia Y. Na+ mechanism of delta-opioid receptor induced protection from anoxic K+ leakage in the cortex. Cell Mol Life Sci. 2009;66:1105-15 pubmed publisher
Pezier A, Bobkov Y, Ache B. The Na+/Ca2+ exchanger inhibitor, KB-R7943, blocks a nonselective cation channel implicated in chemosensory transduction. J Neurophysiol. 2009;101:1151-9 pubmed publisher
Poburko D, Liao C, van Breemen C, Demaurex N. Mitochondrial regulation of sarcoplasmic reticulum Ca2+ content in vascular smooth muscle cells. Circ Res. 2009;104:104-12 pubmed publisher
Xu Y, Tappia P, Goyal R, Dhalla N. Mechanisms of the lysophosphatidic acid-induced increase in [Ca(2+)](i) in skeletal muscle cells. J Cell Mol Med. 2008;12:942-54 pubmed publisher
Baltan S, Besancon E, Mbow B, Ye Z, Hamner M, Ransom B. White matter vulnerability to ischemic injury increases with age because of enhanced excitotoxicity. J Neurosci. 2008;28:1479-89 pubmed publisher
Kansui Y, Garland C, Dora K. Enhanced spontaneous Ca2+ events in endothelial cells reflect signalling through myoendothelial gap junctions in pressurized mesenteric arteries. Cell Calcium. 2008;44:135-46 pubmed publisher
Algara Suárez P, Romero Méndez C, Chrones T, Sánchez Armass S, Meza U, Sims S, et al. Functional coupling between the Na+/Ca2+ exchanger and nonselective cation channels during histamine stimulation in guinea pig tracheal smooth muscle. Am J Physiol Lung Cell Mol Physiol. 2007;293:L191-8 pubmed
Takeuchi A, Tatsumi S, Sarai N, Terashima K, Matsuoka S, Noma A. Ionic mechanisms of cardiac cell swelling induced by blocking Na+/K+ pump as revealed by experiments and simulation. J Gen Physiol. 2006;128:495-507 pubmed
Honda E, Ono K, Kataoka S, Inenaga K. Activation of subfornical organ neurons in rats through pre- and postsynaptic alpha-adrenoceptors. Am J Physiol Regul Integr Comp Physiol. 2006;290:R1646-53 pubmed
Baczkó I, Jones L, McGuigan C, Manning Fox J, Gandhi M, Giles W, et al. Plasma membrane KATP channel-mediated cardioprotection involves posthypoxic reductions in calcium overload and contractile dysfunction: mechanistic insights into cardioplegia. FASEB J. 2005;19:980-2 pubmed
Kohlmeier K, Inoue T, Leonard C. Hypocretin/orexin peptide signaling in the ascending arousal system: elevation of intracellular calcium in the mouse dorsal raphe and laterodorsal tegmentum. J Neurophysiol. 2004;92:221-35 pubmed
Spencer C, Sham J. Effects of Na+/Ca2+ exchange induced by SR Ca2+ release on action potentials and afterdepolarizations in guinea pig ventricular myocytes. Am J Physiol Heart Circ Physiol. 2003;285:H2552-62 pubmed
Su Y, Vacquier V. A flagellar K(+)-dependent Na(+)/Ca(2+) exchanger keeps Ca(2+) low in sea urchin spermatozoa. Proc Natl Acad Sci U S A. 2002;99:6743-8 pubmed publisher
Vines C, Yoshida K, Griffin F, Pillai M, Morisawa M, Yanagimachi R, et al. Motility initiation in herring sperm is regulated by reverse sodium-calcium exchange. Proc Natl Acad Sci U S A. 2002;99:2026-31 pubmed
product information
master code :
1244
SKU :
1244/10
product name :
KB-R7943 mesylate
unit size :
10 mg (also 50 mg)
description :
Na+/Ca2+ exchange inhibitor (reverse mode)
target :
Na+/Ca2+ Exchanger Inhibitors
category :
Small Molecules
purity :
99%
observed molecular weight :
427.49
url print :
?utm_source=labome&utm_medium=referral&utm_campaign=product&utm_term=smallmolecules
details of functionality :
KB-R7943 mesylate is a potent, selective inhibitor of the reverse mode of the Na+/Ca2+ exchanger (IC50 = 0.7 M). Also inhibits the mitochondrial Ca2+ uniporter (MCU; IC50 = 5.5 M). Does not affect Na+-dependent transport systems or ionotropic glutamate receptors.
top caption :
Na+/Ca2+ exchange inhibitor (reverse mode)
extended description :
Na+/Ca2+ exchange inhibitor (reverse mode)
chemical name text :
2-[2-[4-(4-Nitrobenzyloxy)phenyl]ethyl]isothiourea mesylate
formula :
C16H17N3O3S.CH3SO3H
formula text :
C16H17N3O3S.CH3SO3H
cas num :
182004-65-5
USD :
232 USD
product details :
Na+/Ca2+ exchange inhibitor (reverse mode)
storage :
Store at RT
more info or order :
company information
Tocris Bioscience
The Watkins Building
Atlantic Road
Avonmouth, Bristol
BS11 9QD
info@bio-techne.com
https://www.tocris.com
800-343-7475
headquarters: UK