KB-R7943 mesylate

Catalog # Availability Size / Price Qty
1244/10
1244/50
KB-R7943 mesylate | CAS No. 182004-65-5 | Na+/Ca2+ Exchanger Inhibitors
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Description: Na+/Ca2+ exchange inhibitor (reverse mode)

Chemical Name: 2-[2-[4-(4-Nitrobenzyloxy)phenyl]ethyl]isothiourea mesylate

Purity: ≥99%

Product Details
Citations (42)
Reviews (1)

Biological Activity

KB-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.

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.
Tocris products are intended for laboratory research use only, unless stated otherwise.

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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

  1. NCX1 Represents an Ionic Na+ Sensing Mechanism in Macrophages.
    Authors: Neubert Et al.
    PLoS Biol  2020;18
  2. Paraneoplastic cerebellar degeneration: Yo antibody alters mitochondrial calcium buffering capacity.
    Authors: Panja Et al.
    Neuropathol Appl Neurobiol  2019;45:141
  3. Antinociceptive effectiveness of the inhibition of NCX reverse-mode action in rodent neuropathic pain model.
    Authors: Huang Et al.
    Mol Pain  2019;15:1744806919864510
  4. 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
  5. Transient Opening of the Mitochondrial Permeability Transition Pore Induces Microdomain Calcium Transients in Astrocyte Processes.
    Authors: Agarwal Et al.
    Neuron  2017;93:587
  6. 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
  7. Dendritic cell amiloride-sensitive channels mediate sodium-induced inflammation and hypertension.
    Authors: Barbaro
    Cell Rep  2017;21(4):1009
  8. 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
  9. 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
  10. 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
  11. 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
  12. Role of Na+/Ca2+ exchanger in Ca2+ homeostasis in rat suprachiasmatic nucleus neurons.
    Authors: Wang Et al.
    J Neurophysiol  2015;113:2114
  13. An inhibitor of Na(+)/Ca(2+) exchange blocks activation of insect olfactory receptors.
    Authors: Bobkov Et al.
    Biochem Biophys Res Commun  2014;450:1104
  14. 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
  15. 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
  16. Cytosolic calcium coordinates mitochondrial energy metabolism with presynaptic activity.
    Authors: Chouhan Et al.
    J Neurosci  2012;32:1233
  17. 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
  18. 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
  19. 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
  20. Molecular and functional characterization of the human platelet Na(+) /Ca(2+) exchangers.
    Authors: Roberts Et al.
    Br J Pharmacol  2012;165:922
  21. 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
  22. Enhanced Ca(2+)-sensing receptor function in idiopathic pulmonary arterial hypertension.
    Authors: Yamamura Et al.
    Circ Res  2012;111:469
  23. 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
  24. 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
  25. 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
  26. Inhibition of beta-cell sodium-calcium exchange enhances glucose-dependent elevations in cytoplasmic calcium and Ins secretion.
    Authors: Hamming Et al.
    Diabetes  2010;59:1686
  27. Non-cardiomyocytes influence the electrophysiological maturation of human embryonic stem cell-derived cardiomyocytes during differentiation.
    Authors: Kim Et al.
    Sci Rep  2010;19:783
  28. 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
  29. 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
  30. Mitochondrial regulation of sarcoplasmic reticulum Ca2+ content in vascular smooth muscle cells.
    Authors: Poburko Et al.
    Circ Res  2009;104:104
  31. 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
  32. 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
  33. White matter vulnerability to ischemic injury increases with age because of enhanced excitotoxicity.
    Authors: Baltan Et al.
    Stem Cells Dev  2008;28:1479
  34. 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
  35. 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
  36. Activation of subfornical organ neurons in rats through pre- and postsynaptic α-adrenoceptors.
    Authors: Honda Et al.
    Nat Protoc  2006;290:R1646
  37. 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
  38. 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
  39. 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
  40. 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
  41. A flagellar K(+)-dependent Na(+)/Ca(2+) exchanger keeps Ca(2+) low in sea urchin spermatozoa.
    Authors: Su
    Proc Natl Acad Sci U S A  2002;99:6743
  42. 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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All works great!
By Anton Mukhamedshin on 02/18/2019
Application: Species: Human

We use this inhibitor to investigate platelets interaction. We use different concentration to show it activity.The delivery was fast and the product works well


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