Chemical Name: 2-[2-[4-(4-Nitrobenzyloxy)phenyl]ethyl]isothiourea mesylate
Biological ActivityKB-R7943 mesylate is a potent, selective inhibitor of the reverse mode of the Na+/Ca2+ exchanger (IC50 = 0.7 μM). Also inhibits the mitochondrial Ca2+ uniporter (MCU; IC50 = 5.5 μM). Does not affect Na+-dependent transport systems or ionotropic glutamate receptors.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
Reverse Na+/Ca2+ exchange contributes to glutamate-induced intracellular Ca2+ concentration increases in cultured rat forebrain neurons.
Hoyt et al.
The plasma membrane +/Ca2+ exchange inhibitor KB-R7943 is also a potent inhibitor of the mitochondrial Ca2+ uniporter.
Santo-Domingo et al.
The novel Na+/Ca2+ exchange inhibitor KB-R7943 protects CA1 neurons in rat hippocampal slices against hypoxia/hypoglycemic injury.
Schr?der et al.
Effect of +/Ca2+ exchange inhibitor, KB-R7943 on ouabain-induced arrhythmias in guinea-pigs.
Watano et al.
Citations for KB-R7943 mesylate
The citations listed below are publications that use Tocris products. Selected citations for KB-R7943 mesylate include:
42 Citations: Showing 1 - 10
NCX1 Represents an Ionic Na+ Sensing Mechanism in Macrophages.
Authors: Neubert Et al.
PLoS Biol 2020;18
Paraneoplastic cerebellar degeneration: Yo antibody alters mitochondrial calcium buffering capacity.
Authors: Panja Et al.
Neuropathol Appl Neurobiol 2019;45:141
Antinociceptive effectiveness of the inhibition of NCX reverse-mode action in rodent neuropathic pain model.
Authors: Huang Et al.
Mol Pain 2019;15:1744806919864510
Methyl-β-Cyclodextrin Impairs the Phosphorylation of the β2 Subunit of L-Type Calcium Channels and Cytosolic Calcium Homeostasis in Mature Cerebellar Granule Neurons.
Authors: Fortalezas Et al.
Int J Mol Sci 2018;19
Transient Opening of the Mitochondrial Permeability Transition Pore Induces Microdomain Calcium Transients in Astrocyte Processes.
Authors: Agarwal Et al.
KB-R7943 reduces 4-aminopyridine-induced epileptiform activity in adult rats after neuronal damage induced by neonatal monosodium glutamate treatment.
Authors: Hernandez-Ojeda Et al.
J Biomed Sci 2017;24:27
Dendritic cell amiloride-sensitive channels mediate sodium-induced inflammation and hypertension.
Cell Rep 2017;21(4):1009
Transient Oxygen/Glucose Deprivation Causes a Delayed Loss of Mitochondria and Increases Spontaneous Calcium Signaling in Astrocytic Processes.
Authors: O'Donnell Et al.
J Neurosci 2016;36:7109
Transient receptor potential canonical (TRPC)/Orai1-dependent store-operated Ca2+ channels: New targets of aldosterone in cardiomyocytes.
Authors: Sabourin Et al.
Antagonism of Nav channels and α1-adrenergic receptors contributes to vascular smooth muscle effects of ranol.
Authors: Virsolvy Et al.
Am J Physiol Renal Physiol 2015;5:17969
A new mouse model for stationary night blindness with mutant Slc24a1 explains the pathophysiology of the associated human disease.
Authors: Vinberg Et al.
Hum Mol Genet 2015;24:5915
Role of Na+/Ca2+ exchanger in Ca2+ homeostasis in rat suprachiasmatic nucleus neurons.
Authors: Wang Et al.
J Neurophysiol 2015;113:2114
An inhibitor of Na(+)/Ca(2+) exchange blocks activation of insect olfactory receptors.
Authors: Bobkov Et al.
Biochem Biophys Res Commun 2014;450:1104
The effect of high [K(+)]o on spontaneous Ca(2+) waves in freshly isolated interstitial cells of Cajal from the rabbit urethra.
Authors: Drumm Et al.
Physiol Rep 2014;2:e00203
R.zole and gabapentinoids activate glutamate transporters to facilitate glutamate-induced glutamate release from cultured astrocytes.
Authors: Yoshizumi Et al.
Eur J Pharmacol 2012;677:87
Cytosolic calcium coordinates mitochondrial energy metabolism with presynaptic activity.
Authors: Chouhan Et al.
J Neurosci 2012;32:1233
Pro-death and pro-survival properties of ouabain in U937 lymphoma derived cells.
Authors: Cuozzo Et al.
J Exp Clin Cancer Res 2012;31:95
The epithelial sodium/proton exchanger, NHE3, is necessary for renal and intestinal calcium (re)absorption.
Authors: Pan Et al.
Biochem Biophys Res Commun 2012;302:F943
Na delivery and ENaC mediate flow regulation of collecting duct endothelin-1 production.
Authors: Pandit Et al.
Am J Physiol Renal Physiol 2012;302:F1325
Molecular and functional characterization of the human platelet Na(+) /Ca(2+) exchangers.
Authors: Roberts Et al.
Br J Pharmacol 2012;165:922
High potency inhibition of hERG potassium channels by the sodium-calcium exchange inhibitor KB-R7943.
Authors: Cheng Et al.
Br J Pharmacol 2012;165:2260
Enhanced Ca(2+)-sensing receptor function in idiopathic pulmonary arterial hypertension.
Authors: Yamamura Et al.
Circ Res 2012;111:469
Inhibition of spontaneous activity of rabbit atrioventricular node cells by KB-R7943 and inhibitors of sarcoplasmic reticulum Ca(2+) ATPase.
Authors: Cheng Et al.
Cell Calcium 2011;49:56
Mechanistic distinction between activation and inhibition of (Na(+)+K(+))-ATPase-mediated Ca2+ influx in cardiomyocytes.
Authors: Xu Et al.
Proc Natl Acad Sci U S A 2011;406:200
PKC-dependent coupling of calcium permeation through transient receptor potential canonical 3 (TRPC3) to calcineurin signaling in HL-1 myocytes.
Authors: Poteser Et al.
Am J Physiol Regul Integr Comp Physiol 2011;108:10556
Inhibition of beta-cell sodium-calcium exchange enhances glucose-dependent elevations in cytoplasmic calcium and Ins secretion.
Authors: Hamming Et al.
Non-cardiomyocytes influence the electrophysiological maturation of human embryonic stem cell-derived cardiomyocytes during differentiation.
Authors: Kim Et al.
Sci Rep 2010;19:783
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.
Authors: Barrientos Et al.
Mol Pharmacol 2009;76:560
Na+ mechanism of delta-opioid receptor induced protection from anoxic K+ leakage in the cortex.
Authors: Chao Et al.
Cell Mol Life Sci 2009;66:1105
Mitochondrial regulation of sarcoplasmic reticulum Ca2+ content in vascular smooth muscle cells.
Authors: Poburko Et al.
Circ Res 2009;104:104
The Na+/Ca2+ exchanger inhibitor, KB-R7943, blocks a nonselective cation channel implicated in chemosensory transduction.
Authors: Pezier Et al.
J Neurophysiol 2009;101:1151
Enhanced spontaneous Ca2+ events in endothelial cells reflect signalling through myoendothelial gap junctions in pressurized mesenteric arteries.
Authors: Kansui Et al.
Cell Calcium 2008;44:135
White matter vulnerability to ischemic injury increases with age because of enhanced excitotoxicity.
Authors: Baltan Et al.
Stem Cells Dev 2008;28:1479
Mechanisms of the lysophosphatidic acid-induced increase in [Ca(2+)](i) in skeletal muscle cells.
Authors: Xu Et al.
J Cell Mol Med 2008;12:942
Functional coupling between the Na+/Ca2+ exchanger and nonselective cation channels during histamine stimulation in guinea pig tracheal smooth muscle.
Authors: Algara-Suárez Et al.
Am J Physiol Lung Cell Mol Physiol 2007;293:L191
Activation of subfornical organ neurons in rats through pre- and postsynaptic α-adrenoceptors.
Authors: Honda Et al.
Nat Protoc 2006;290:R1646
Ionic mechanisms of cardiac cell swelling induced by blocking Na+/K+ pump as revealed by experiments and simulation.
Authors: Takeuchi Et al.
J Gen Physiol 2006;128:495
Plasma membrane KATP channel-mediated cardioprotection involves posthypoxic reductions in calcium overload and contractile dysfunction: mechanistic insights into cardioplegia.
Authors: Baczkó Et al.
FASEB J 2005;19:980
Hypocretin/orexin peptide signaling in the ascending arousal system: elevation of intracellular calcium in the mouse dorsal raphe and laterodorsal tegmentum.
Authors: Kohlmeier Et al.
J Neurophysiol 2004;92:221
Effects of Na+/Ca2+ exchange induced by SR Ca2+ release on action potentials and afterdepolarizations in guinea pig ventricular myocytes.
Authors: Spencer and Sham
Am J Physiol Heart Circ Physiol 2003;285:H2552
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
Motility initiation in herring sperm is regulated by reverse sodium-calcium exchange.
Authors: Vines Et al.
Proc Natl Acad Sci U S A 2002;99:2026
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