KB-R7943 mesylate

• CAT Number: I002362
• CAS Number: 182004-65-5
• Molecular Formula: C16H17N3O3S • CH3SO3H
• Molecular Weight: 427.5
• Purity: ≥95%
• Target: Na+/Ca2+ Exchanger
• Solubility: H2O: ≤ 4.3 mg/mL (Need warming)
• Storage: 2-8°C
• IC50: 0.7 mM
• IUPAC Name: methanesulfonic acid;2-[4-[(4-nitrophenyl)methoxy]phenyl]ethyl carbamimidothioate
• InChI: 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)
• InChIKey: WGIKEBHIKKWJLG-UHFFFAOYSA-N
• SMILES: CS(=O)(=O)O.C1=CC(=CC=C1CCSC(=N)N)OCC2=CC=C(C=C2)[N+](=O)[O-]

KB-R7943 mesylate（Cat No.:I002362） is a potent and selective inhibitor of the reverse mode of the Na+/Ca2+ exchanger. With an IC50 value of 0.7 mM, it effectively inhibits the activity of the Na+/Ca2+ exchanger in this mode. By blocking the reverse mode of the Na+/Ca2+ exchanger, KB-R7943 mesylate disrupts the regulation of intracellular calcium levels, which has implications for various physiological and pathological processes. This compound serves as a valuable tool for studying the role of the Na+/Ca2+ exchanger and its potential as a therapeutic target in calcium-related disorders.

Reference

[1]. Cheng, Hongwei; Zhang, Yihong; Du, Chunyun et al. High potency inhibition of hERG potassium channels by the sodium-calcium exchange inhibitor KB-R7943. British Journal of Pharmacology (2012), 165(7), 2260-2273.
[2]. Talbot, Janet D.; David, Gavriel; Barrett, Ellen F.; Barrett, John N. Calcium dependence of damage to mouse motor nerve terminals following oxygen/glucose deprivation. Experimental Neurology (2012), 234(1), 95-104.
[3]. Brustovetsky, Tatiana; Brittain, Matthew K.; Sheets, Patrick L. et al. KB-R7943, an inhibitor of the reverse Na+/Ca2+ exchanger, blocks N-methyl–aspartate receptor and inhibits mitochondrial complex I. British Journal of Pharmacology (2010), Volume Date2011, 162(1), 255-270.
[4]. Barrientos, Genaro; Bose, Diptiman D.; Feng, Wei The Na+/Ca2+ exchange inhibitor 2-(2-(4-(4-nitrobenzyloxy)phenyl)ethyl)isothiourea methanesulfonate (KB-R7943) also blocks ryanodine receptors type 1 (RyR1) and type 2 (RyR2) channels. Molecular Pharmacology (2009), 76(3), 560-568.
[5]. Storozhevykh, T. P.; Senilova, Ya. E.; Brustovetsky, T. et al. Neuroprotective Effect of KB-R7943 Against Glutamate Excitotoxicity is Related to Mild Mitochondrial Depolarization. Neurochemical Research (2010), 35(2), 323-335.
[6]. MacDonald, Ashley C.; Howlett, Susan E. Differential effects of the sodium calcium exchange inhibitor, KB-R7943, on ischemia and reperfusion injury in isolated guinea pig ventricular myocytes. European Journal of Pharmacology (2008), 580(1-2), 214-223.