KB-R7943 mesylate
TRPC channel blocker / KB-R7943 is a potent and selective inhibitor of the reversed Na+/Ca2+ exchanger (NCE or NCX; IC50’s = 1.2-2.4 µM in cardiomyocytes, smooth muscle cells, NCX1-transfected fibroblasts1; 0.7µM in cultured rat forebrain2). KB-R7943 has also been shown to inhibit the mitochondrial Ca2+ uniporter (MCU) – Ki = 5.5 µM.3 Recently shown to inhibit complex I in the mitochondrial respiratory chain (IC50 = 11.4 µM) and block NMDA receptors (IC50 = 13.4 µM).4
Biochemicals & reagents
182004-65-5
1) Iwamoto et al. (1996), Novel Isothioures Derivative Selectively Inhibits the Reverse Mode of Na+/Ca2+ Exchange in Cells Expressing NCX1. J.Biol.Chem., 271 22391 / 2) 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 / 3) Santo-Domingo et al. (2007) The plasma membrane Na+/Ca2+ exchange inhibitor KB-R7943 is also a potent inhibitor of the mitochondrial Ca2+ uniporter. Br.J.Pharmacol. 151 647 / 4) Brustovetsky et al. (2011) KB-R7943, an inhibitor of the reverse Na+/Ca2+ exchanger, blocks N-methyl-D-aspartate receptor and inhibits mitochondrial complex I. Br.J.Pharmacol. 162 255
RT
TARGET: Ion channel -- PATHWAY: Calcium signaling; Mitochondrial function