KB-R7943 mesylate

Cat. No. 1244

KB-R7943 mesylate C16H17N3O3S.CH3SO3H [182004-65-5]

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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.

Certificate of Analysis / Product Datasheet / Safety Data Sheet

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.

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.

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

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

Poburko et al (2009) Mitochondrial regulation of sarcoplasmic reticulum Ca2+ content in vascular smooth muscle cells. Circ Res 104 104. PMID: 19023135.

Baltan et al (2008) White matter vulnerability to ischemic injury increases with age because of enhanced excitotoxicity. Stem Cells Dev 28 1479. PMID: 18256269.

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.

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.

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.

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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, Tocris Bioscience, Na+/Ca2+ Exchanger Inhibitor products

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