Product Overview
KB-R7943 mesylate is a potent and selective inhibitor of Na+/Ca2+ exchanger (NCE) with IC50 value of 0.7 μM. NCE is an antiporter membrane protein that exchanges 3 Na+ for 1 Ca2+ and can function to cause Ca2+ accumulation (reverse mode) or Ca2+ extrusion (forward mode) depending on the concentrations of each ion on either side of the membrane and on the membrane potential. In transfected Chinese hamster ovary (CHO) cells expressing NCE, KB-R7943 (10 μM) inhibited NCX activity at high (140mM) but not at low (10mM) cytosolic Na+ concentrations. In cultured rat forebrain neurons loaded with glutamate-(3 μM), N-methyl-D-aspartate-(30 μM), kainate-(100 μM) or KCl-(50 mM) induced [Ca2+] transients, KBR7943 inhibited these transients with IC50 values of 6.6, 8.2, 5.2 and 2.9 μM, respectively. While, KB-R7943 didn't inhibit glutamate-induced neuronal injury. In mice with ischemic acute renal failure (ARF), KB-R7943 significantly decreased endothelin-1 (ET-1) in the kidney and relieved the ARF-induced renal dysfunction.