Shelf life (days): 1460.0
Formulation: A crystalline solid
Formal Name: carbamimidothioic acid, 2-[4-[(4-nitrophenyl)methoxy]phenyl]ethyl ester, monomethanesulfonate
Purity: ≥98%
Formula Markup: C16H17N3O3S / CH3SO3H
Formula Weight: 427.5
CAS Number: 182004-65-5
Notes: The Na+/Ca2+ exchanger (NCX) is a major regulator of intracellular calcium concentration that is largely expressed in cardiac sarcolemma (NCX1) but also in brain and skeletal muscle (NCX2). KB-R7943 is an isothiourea derivative that selectively inhibits the reverse mode of NCX1 (IC50 = 1.2-2.4 µM), preventing intracellular sodium-dependent calcium uptake in whole cells.{26636} It is much less potent at preventing extracellular sodium-dependent calcium efflux from intact cells (IC50 > 30 µM).{26636} In cultured hippocampal neurons, KB-R7943 exhibits neuroprotection from glutamate-induced excitotoxicity by blocking NMDA receptor-mediated activity (IC50 = 13.4 µM) and inhibiting complex I in the mitochondrial respiratory chain (IC50 = 11.4 µM).{26637} KB-R7943 has also been shown to block transient receptor potential canonical channels, which are important mediators of calcium-dependent signal transduction.{26638}
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