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Submit ReviewKB-R7943 mesylate
Description: Na+/Ca2+ exchange inhibitor (reverse mode)
Chemical Name: 2-[2-[4-(4-Nitrobenzyloxy)phenyl]ethyl]isothiourea mesylate
Purity: ≥99% (HPLC)
Biological Activity for KB-R7943 mesylate
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.
Compound Libraries for KB-R7943 mesylate
KB-R7943 mesylate is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for KB-R7943 mesylate
| M. Wt | 427.49 |
| Formula | C16H17N3O3S.CH3SO3H |
| Storage | Store at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 182004-65-5 |
| PubChem ID | 9823846 |
| InChI Key | WGIKEBHIKKWJLG-UHFFFAOYSA-N |
| Smiles | CS(O)(=O)=O.NC(=N)SCCC1=CC=C(OCC2=CC=C(C=C2)[N+]([O-])=O)C=C1 |
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.
Solubility Data for KB-R7943 mesylate
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 42.75 | 100 |
Preparing Stock Solutions for KB-R7943 mesylate
The following data is based on the product molecular weight 427.49. 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 | 2.34 mL | 11.7 mL | 23.39 mL |
| 5 mM | 0.47 mL | 2.34 mL | 4.68 mL |
| 10 mM | 0.23 mL | 1.17 mL | 2.34 mL |
| 50 mM | 0.05 mL | 0.23 mL | 0.47 mL |
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Product Datasheets for KB-R7943 mesylate
References for KB-R7943 mesylate
References are publications that support the biological activity of the product.
Hoyt et al (1998) Reverse Na+/Ca2+ exchange contributes to glutamate-induced intracellular Ca2+ concentration increases in cultured rat forebrain neurons. Mol.Pharmacol. 53 742 PMID: 9547366
Santo-Domingo et al (2007) The plasma membrane +/Ca2+ exchange inhibitor KB-R7943 is also a potent inhibitor of the mitochondrial Ca2+ uniporter. Br.J.Pharmacol. 151 647 PMID: 17471180
Schröder et al (1999) The novel Na+/Ca2+ exchange inhibitor KB-R7943 protects CA1 neurons in rat hippocampal slices against hypoxia/hypoglycemic injury. Neuropharmacology 38 319 PMID: 10218875
Watano et al (1999) Effect of +/Ca2+ exchange inhibitor, KB-R7943 on ouabain-induced arrhythmias in guinea-pigs. Br.J.Pharmacol. 127 1846 PMID: 10482915
If you know of a relevant reference for KB-R7943 mesylate, please let us know.
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Keywords: KB-R7943 mesylate, KB-R7943 mesylate supplier, Na+/Ca2+, exchange, inhibitors, reverse, mode, inhibits, Sodium, Calcium, Exchanger, Ion, Transporters, Pumps, Ca2+, Signaling, Signalling, NCX, Mitochondrial, Uniporter, 1244, Tocris Bioscience
42 Citations for KB-R7943 mesylate
Citations are publications that use Tocris products. Selected citations for KB-R7943 mesylate include:
Panja et al (2019) Paraneoplastic cerebellar degeneration: Yo antibody alters mitochondrial calcium buffering capacity. Neuropathol Appl Neurobiol 45 141 PMID: 29679372
O'Donnell et al (2016) Transient Oxygen/Glucose Deprivation Causes a Delayed Loss of Mitochondria and Increases Spontaneous Calcium Signaling in Astrocytic Processes. J Neurosci 36 7109 PMID: 27383588
Sabourin et al (2016) Transient receptor potential canonical (TRPC)/Orai1-dependent store-operated Ca2+ channels: New targets of aldosterone in cardiomyocytes. J.Biol.Chem. 291 13394 PMID: 27129253
Virsolvy et al (2015) Antagonism of Nav channels and α1-adrenergic receptors contributes to vascular smooth muscle effects of ranol. Am J Physiol Renal Physiol 5 17969 PMID: 26655634
Drumm et al (2014) The effect of high [K(+)]o on spontaneous Ca(2+) waves in freshly isolated interstitial cells of Cajal from the rabbit urethra. Physiol Rep 2 e00203 PMID: 24744882
Bobkov et al (2014) An inhibitor of Na(+)/Ca(2+) exchange blocks activation of insect olfactory receptors. Biochem Biophys Res Commun 450 1104 PMID: 24996179
Kim et al (2010) Non-cardiomyocytes influence the electrophysiological maturation of human embryonic stem cell-derived cardiomyocytes during differentiation. Sci Rep 19 783 PMID: 20001453
Huang et al (2019) Antinociceptive effectiveness of the inhibition of NCX reverse-mode action in rodent neuropathic pain model. Mol Pain 15 1744806919864510 PMID: 31370728
Barbaro (2017) Dendritic cell amiloride-sensitive channels mediate sodium-induced inflammation and hypertension. Cell Rep 21 1009 PMID: 29069584
Hernandez-Ojeda et al (2017) KB-R7943 reduces 4-aminopyridine-induced epileptiform activity in adult rats after neuronal damage induced by neonatal monosodium glutamate treatment. J Biomed Sci 24 27 PMID: 28486943
Pan et al (2012) The epithelial sodium/proton exchanger, NHE3, is necessary for renal and intestinal calcium (re)absorption. Biochem Biophys Res Commun 302 F943 PMID: 21937605
Xu et al (2011) Mechanistic distinction between activation and inhibition of (Na(+)+K(+))-ATPase-mediated Ca2+ influx in cardiomyocytes. Proc Natl Acad Sci U S A 406 200 PMID: 21303662
Poteser et al (2011) PKC-dependent coupling of calcium permeation through transient receptor potential canonical 3 (TRPC3) to calcineurin signaling in HL-1 myocytes. Am J Physiol Regul Integr Comp Physiol 108 10556 PMID: 21653882
Cheng et al (2011) Inhibition of spontaneous activity of rabbit atrioventricular node cells by KB-R7943 and inhibitors of sarcoplasmic reticulum Ca(2+) ATPase. Cell Calcium 49 56 PMID: 21163524
Baltan et al (2008) White matter vulnerability to ischemic injury increases with age because of enhanced excitotoxicity. Stem Cells Dev 28 1479 PMID: 18256269
Vinberg et al (2015) A new mouse model for stationary night blindness with mutant Slc24a1 explains the pathophysiology of the associated human disease. Hum Mol Genet 24 5915 PMID: 26246500
Poburko et al (2009) Mitochondrial regulation of sarcoplasmic reticulum Ca2+ content in vascular smooth muscle cells. Circ Res 104 104 PMID: 19023135
Chao et al (2009) Na+ mechanism of delta-opioid receptor induced protection from anoxic K+ leakage in the cortex. Cell Mol Life Sci 66 1105 PMID: 19189047
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
Fortalezas et al (2018) 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 19 PMID: 30463327
Wang et al (2015) Role of Na+/Ca2+ exchanger in Ca2+ homeostasis in rat suprachiasmatic nucleus neurons. J Neurophysiol 113 2114 PMID: 25568156
Yoshizumi et al (2012) R.zole and gabapentinoids activate glutamate transporters to facilitate glutamate-induced glutamate release from cultured astrocytes. Eur J Pharmacol 677 87 PMID: 22206816
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
Chouhan et al (2012) Cytosolic calcium coordinates mitochondrial energy metabolism with presynaptic activity. J Neurosci 32 1233 PMID: 22279208
Roberts et al (2012) Molecular and functional characterization of the human platelet Na(+) /Ca(2+) exchangers. Br J Pharmacol 165 922 PMID: 21790537
Hamming et al (2010) Inhibition of beta-cell sodium-calcium exchange enhances glucose-dependent elevations in cytoplasmic calcium and Ins secretion. Diabetes 59 1686 PMID: 20413506
Neubert et al (2020) NCX1 Represents an Ionic Na+ Sensing Mechanism in Macrophages. PLoS Biol 18 PMID: 32569301
Agarwal et al (2017) Transient Opening of the Mitochondrial Permeability Transition Pore Induces Microdomain Calcium Transients in Astrocyte Processes. Neuron 93 587 PMID: 28132831
Cheng et al (2012) High potency inhibition of hERG potassium channels by the sodium-calcium exchange inhibitor KB-R7943. Br J Pharmacol 165 2260 PMID: 21950687
Pandit et al (2012) Na delivery and ENaC mediate flow regulation of collecting duct endothelin-1 production. Am J Physiol Renal Physiol 302 F1325 PMID: 22357920
Yamamura et al (2012) Enhanced Ca(2+)-sensing receptor function in idiopathic pulmonary arterial hypertension. Circ Res 111 469 PMID: 22730443
Cuozzo et al (2012) Pro-death and pro-survival properties of ouabain in U937 lymphoma derived cells. J Exp Clin Cancer Res 31 95 PMID: 23153195
Honda et al (2006) Activation of subfornical organ neurons in rats through pre- and postsynaptic α-adrenoceptors. Nat Protoc 290 R1646 PMID: 16455764
Algara-Suárez et al (2007) 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 293 L191 PMID: 17449794
Xu et al (2008) Mechanisms of the lysophosphatidic acid-induced increase in [Ca(2+)](i) in skeletal muscle cells. J Cell Mol Med 12 942 PMID: 18494935
Kansui et al (2008) Enhanced spontaneous Ca2+ events in endothelial cells reflect signalling through myoendothelial gap junctions in pressurized mesenteric arteries. Cell Calcium 44 135 PMID: 18191200
Kohlmeier et al (2004) Hypocretin/orexin peptide signaling in the ascending arousal system: elevation of intracellular calcium in the mouse dorsal raphe and laterodorsal tegmentum. J Neurophysiol 92 221 PMID: 14999052
Spencer and Sham (2003) 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 285 H2552 PMID: 12933341
Vines et al (2002) Motility initiation in herring sperm is regulated by reverse sodium-calcium exchange. Proc Natl Acad Sci U S A 99 2026 PMID: 11842223
Su (2002) A flagellar K(+)-dependent Na(+)/Ca(2+) exchanger keeps Ca(2+) low in sea urchin spermatozoa. Proc Natl Acad Sci U S A 99 6743 PMID: 12011436
Baczkó et al (2005) Plasma membrane KATP channel-mediated cardioprotection involves posthypoxic reductions in calcium overload and contractile dysfunction: mechanistic insights into cardioplegia. FASEB J 19 980 PMID: 15774423
Takeuchi et al (2006) Ionic mechanisms of cardiac cell swelling induced by blocking Na+/K+ pump as revealed by experiments and simulation. J Gen Physiol 128 495 PMID: 17074975
Do you know of a great paper that uses KB-R7943 mesylate from Tocris? Please let us know.
Reviews for KB-R7943 mesylate
Average Rating: 5 (Based on 1 Review.)
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All works great!.
By
Anton Mukhamedshin on 02/18/2019
Assay Type: Ex Vivo
Species: Human
Cell Line/Tissue: Platelets
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