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.
|Storage||Store at RT|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 427.49. Batch specific molecular weights may vary from batch to batch due to solvent 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|
References are publications that support the products' biological activity.
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, supplier, Na+/Ca2+, exchange, inhibitors, reverse, mode, inhibits, Sodium, Calcium, Exchanger, Ion, Transporters, Pumps, Ca2+, Signaling, Signalling, NCX, Na+/Ca2+, Exchanger, Mitochondrial, Calcium, Uniporter, Na+/Ca2+, Exchanger, Tocris Bioscience
20 Citations for KB-R7943 mesylate
Citations are publications that use Tocris products. Selected citations for KB-R7943 mesylate include:
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
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
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
Barbaro (2017) Dendritic cell amiloride-sensitive channels mediate sodium-induced inflammation and hypertension. Cell Rep 21 1009 PMID: 29069584
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 ranolazine. Am J Physiol Renal Physiol 5 17969 PMID: 26655634
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
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
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
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
Baltan et al (2008) White matter vulnerability to ischemic injury increases with age because of enhanced excitotoxicity. Stem Cells Dev 28 1479 PMID: 18256269
Honda et al (2006) Activation of subfornical organ neurons in rats through pre- and postsynaptic α-adrenoceptors. Nat Protoc 290 R1646 PMID: 16455764
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
Do you know of a great paper that uses KB-R7943 mesylate from Tocris? If so please let us know.
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