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KB-R7943 mesylate

Cat No.
CEI-1385
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.
CAS No.
182004-65-5
Molecular Weight
427.5
Purity
0.98
Storage
Store at -20°C
Synonyms
KB-R7943; KB-R 7943
Targets
NCE
Molecular Formula
C17H21N3O6S2
Chemical Name
methanesulfonic acid; 2-[4-[(4-nitrophenyl)methoxy]phenyl]ethyl carbamimidothioate
Solubility
Soluble in DMSO > 10 mM
Shipping Conditions
Evaluation sample solution: ship with blue ice. All other available size: ship with RT, or blue ice upon request
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