Catalog Number: 1244
Chemical Name: 2-[2-[4-(4-Nitrobenzyloxy)phenyl]ethyl]isothiourea mesylate
Biological Activity
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.
Technical Data
  • M.Wt:
    427.49
  • Formula:
    C16H17N3O3S.CH3SO3H
  • Solubility:
    Soluble to 100 mM in DMSO
  • Purity:
    >99%
  • Storage:
    Store at RT
  • CAS No:
    182004-65-5
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. Reverse Na+/Ca2+ exchange contributes to glutamate-induced intracellular Ca2+ concentration increases in cultured rat forebrain neurons.
    Hoyt et al.
    Mol.Pharmacol., 1998;53:742
  2. The plasma membrane +/Ca2+ exchange inhibitor KB-R7943 is also a potent inhibitor of the mitochondrial Ca2+ uniporter.
    Santo-Domingo et al.
    Br.J.Pharmacol., 2007;151:647
  3. The novel Na+/Ca2+ exchange inhibitor KB-R7943 protects CA1 neurons in rat hippocampal slices against hypoxia/hypoglycemic injury.
    Schr?der et al.
    Neuropharmacology, 1999;38:319
  4. Effect of +/Ca2+ exchange inhibitor, KB-R7943 on ouabain-induced arrhythmias in guinea-pigs.
    Watano et al.
    Br.J.Pharmacol., 1999;127:1846
Citations:

The citations listed below are publications that use Tocris products. Selected citations for KB-R7943 mesylate include:

20 Citations: Showing 1 - 10
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  1. Dendritic cell amiloride-sensitive channels mediate sodium-induced inflammation and hypertension.
    Authors: Barbaro
    Cell?Rep 2017;21(4):1009
  2. Transient receptor potential canonical (TRPC)/Orai1-dependent store-operated Ca2+ channels: New targets of aldosterone in cardiomyocytes.
    Authors: Sabourin Et al.
    J.Biol.Chem. 2016;291:13394
  3. Antagonism of Nav channels and α1-adrenergic receptors contributes to vascular smooth muscle effects of ranolazine.
    Authors: Virsolvy Et al.
    Am J Physiol Renal Physiol 2015;5:17969
  4. 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
  5. 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
  6. 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
  7. 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
  8. Enhanced Ca(2+)-sensing receptor function in idiopathic pulmonary arterial hypertension.
    Authors: Yamamura Et al.
    Circ Res 2012;111:469
  9. 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
  10. 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
  11. 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
  12. Non-cardiomyocytes influence the electrophysiological maturation of human embryonic stem cell-derived cardiomyocytes during differentiation.
    Authors: Kim Et al.
    Sci Rep 2010;19:783
  13. 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
  14. 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
  15. Mitochondrial regulation of sarcoplasmic reticulum Ca2+ content in vascular smooth muscle cells.
    Authors: Poburko Et al.
    Circ Res 2009;104:104
  16. 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
  17. White matter vulnerability to ischemic injury increases with age because of enhanced excitotoxicity.
    Authors: Baltan Et al.
    Stem Cells Dev 2008;28:1479
  18. 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
  19. Activation of subfornical organ neurons in rats through pre- and postsynaptic α-adrenoceptors.
    Authors: Honda Et al.
    Nat Protoc 2006;290:R1646
  20. 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
Expand to show all 20 Citations

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