KB-R7943 (mesylate)

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. It is much less potent at preventing extracellular sodium-dependent calcium efflux from intact cells (IC50 > 30 µM). 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). KB-R7943 has also been shown to block transient receptor potential canonical channels, which are important mediators of calcium-dependent signal transduction.Formal Name: carbamimidothioic acid, 2-[4-[(4-nitrophenyl)methoxy]phenyl]ethyl ester, monomethanesulfonate. CAS Number: 182004-65-5. Molecular Formula: C16H17N3O3S . CH3SO3H. Formula Weight: 427.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml. lambdamax: 223, 269 nm. SMILES: NC(SCCC(C=C1)=CC=C1OCC2=CC=C([N+]([O-])=O)C=C2)=N.OS(C)(=O)=O. InChi Code: InChI=1S/C16H17N3O3S.CH4O3S/c17-16(18)23-10-9-12-3-7-15(8-4-12)22-11-13-1-5-14(6-2-13)19(20)21,1-5(2,3)4/h1-8H,9-11H2,(H3,17,18),1H3,(H,2,3,4). InChi Key: WGIKEBHIKKWJLG-UHFFFAOYSA-N.