KB-R7943 MESYLATE (CAS 182004-65-5)
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KB-R7943 mesylate is a cell permeable, potent, selective NCKX inhibitor of the reverse mode of Na+/Ca2+ exchange in cells expressing NCX1. NCX1 is a Na+/Ca2+ exchanger predominantly expressed in cardiac sarcolemma, as well as in brain, kidney, liver, pancreas, skeletal muscle, placenta and lung. NCX1 expression is up-regualted in human heart failure, as well as in other animal heart failure models. KB-R7943 reversibly inhibits inward and outward Na+/Ca2+ exchange in a dose-dependent manner, although it inhibits outward exchange more potently. Non-competitive with respect to Na+/Ca2+ and exhibits neuroprotection against glutamate excitotoxicity in rat cultured cerebellar granule neurons. KB-R7943 suppressed ventricular arrhythmias (tachycardia and fibrillation) associated with both ischemia and reperfusion almost completely in a rabbit ischemia-reperfusion model of cardiac injury. KB-R7943 is also a potent blocker of the transient receptor potential channels (TRPC) TRPC3, TRPC5 and TRPC6. KB-R7943 MESYLATE is an inhibitor of NCX1, NCX2, NCX3 and CCDC109. KB-R7943 mesylate specifically targets the reverse mode of the sodium/calcium exchanger, which is responsible for the extrusion of calcium ions from the cell.
KB-R7943 MESYLATE (CAS 182004-65-5) References
- Inhibition of Na+/Ca2+ exchange by KB-R7943: transport mode selectivity and antiarrhythmic consequences. | Elias, CL., et al. 2001. Am J Physiol Heart Circ Physiol. 281: H1334-45. PMID: 11514305
- The Na+/Ca2+ exchange inhibitor KB-R7943 potently blocks TRPC channels. | Kraft, R. 2007. Biochem Biophys Res Commun. 361: 230-6. PMID: 17658472
- The Na+/Ca2+ exchanger inhibitor, KB-R7943, blocks a nonselective cation channel implicated in chemosensory transduction. | Pezier, A., et al. 2009. J Neurophysiol. 101: 1151-9. PMID: 19118110
- 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. | Barrientos, G., et al. 2009. Mol Pharmacol. 76: 560-8. PMID: 19509218
- Chronic administration of KB-R7943 induces up-regulation of cardiac NCX1. | Xu, L., et al. 2009. J Biol Chem. 284: 27265-72. PMID: 19661061
- Neuroprotective effect of KB-R7943 against glutamate excitotoxicity is related to mild mitochondrial depolarization. | Storozhevykh, TP., et al. 2010. Neurochem Res. 35: 323-35. PMID: 19771515
- KB-R7943 inhibits high glucose-induced endothelial ICAM-1 expression and monocyte-endothelial adhesion. | Li, J., et al. 2010. Biochem Biophys Res Commun. 392: 516-9. PMID: 20096662
- Hypervariable intronic region in NCX1 is enriched in short insertion-deletion polymorphisms and showed association with cardiovascular traits. | Kepp, K., et al. 2010. BMC Med Genet. 11: 15. PMID: 20109173
- Inhibition of sodium-calcium exchange by KB-R7943: Dodecylamine and sphingosine in transfected Chinese hamster ovary cells. | Condrescu, M. and Reeves, JP. 2010. Cell Calcium. 47: 404-11. PMID: 20206994
- Inhibition of beta-cell sodium-calcium exchange enhances glucose-dependent elevations in cytoplasmic calcium and insulin secretion. | Hamming, KS., et al. 2010. Diabetes. 59: 1686-93. PMID: 20413506
- Inhibition of the cardiac ATP-dependent potassium current by KB-R7943. | Abramochkin, DV. and Vornanen, M. 2014. Comp Biochem Physiol A Mol Integr Physiol. 175: 38-45. PMID: 24845199
- A novel isothiourea derivative selectively inhibits the reverse mode of Na+/Ca2+ exchange in cells expressing NCX1. | Iwamoto, T., et al. 1996. J Biol Chem. 271: 22391-7. PMID: 8798401
- A novel antagonist, No. 7943, of the Na+/Ca2+ exchange current in guinea-pig cardiac ventricular cells. | Watano, T., et al. 1996. Br J Pharmacol. 119: 555-63. PMID: 8894178
Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
KB-R7943 MESYLATE, 10 mg | sc-202681 | 10 mg | $157.00 |