KB-R7943 mesylate
Catalog #:
IN0038Shipping advice:
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| IN0038-10mg | USD109.0 |
| IN0038-50mg | USD499.0 |
Synomyms: KB-R7943 mesylate
IUPAC Name:
2-[2-[4-(4-Nitrobenzyloxy)phenyl]ethyl]isothiourea mesylateFunctional Activity:
This is a potent and selective inhibitor of the reverse mode of the Na+/Ca2+ exchanger (IC50 = 0.7 mM). It also inhibits the mitochondrial Ca2+ uniporter (MCU; IC50 = 5.5 μM). It was shown not to affect Na+-dependent transport systems or ionotropic glutamate receptors.Technical Data:
M.Wt: 427.49
Formula: C16H17N3O3S.CH3SO3H
Solubility: Soluble to 100 mM in DMSO
Purity: >99%
Storage: Store at room temperature
CAS No.: 182004-65-5
Related Products by Target:
NCX Monoclonal Antibody
Solubility: Soluble to 100 mM in DMSO
Purity: >99%
Storage: Store at room temperature
CAS No.: 182004-65-5
Related Products by Target:
NCX Monoclonal Antibody
Storage: Store at room temperature
CAS No.: 182004-65-5
Related Products by Target:
NCX Monoclonal Antibody
Related Products by Target:
NCX Monoclonal AntibodyReferences for KB-R7943:
1. Storozhevykh, T. P., Senilova, Y. E., Brustovetsky, T., Pinelis, V. G., and Brustovetsky, N. Neuroprotective effect of KB-R7943 against glutamate excitotoxicity is related to mild mitochondrial depolarization. Neurochem Res, 35: 323-335.
2. Xu, L., Kappler, C. S., Mani, S. K., Shepherd, N. R., Renaud, L., Snider, P., Conway, S. J., and Menick, D. R. Chronic administration of KB-R7943 induces up-regulation of cardiac NCX1. J Biol Chem, 284: 27265-27272, 2009.
3. Barrientos, G., Bose, D. D., Feng, W., Padilla, I., and Pessah, I. N. 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. Mol Pharmacol, 76: 560-568, 2009.
4. Pezier, A., Bobkov, Y. V., and Ache, B. W. The Na+/Ca2+ exchanger inhibitor, KB-R7943, blocks a nonselective cation channel implicated in chemosensory transduction. J Neurophysiol, 101: 1151-1159, 2009.
5. Santo-Domingo, J., Vay, L., Hernandez-Sanmiguel, E., Lobaton, C. D., Moreno, A., Montero, M., and Alvarez, J. The plasma membrane Na+/Ca2+ exchange inhibitor KB-R7943 is also a potent inhibitor of the mitochondrial Ca2+ uniporter. Br J Pharmacol, 151: 647-654, 2007.
6. Shinada, T., Hirayama, Y., Maruyama, M., Ohara, T., Yashima, M., Kobayashi, Y., Atarashi, H., and Takano, T. Inhibition of the reverse mode of the Na+/Ca2+ exchange by KB-R7943 augments arrhythmogenicity in the canine heart during rapid heart rates. J Electrocardiol, 38: 218-225, 2005.
7. Takano, S., Kimura, J., and Ono, T. Inhibition of aggregation of rabbit and human platelets induced by adrenaline and 5-hydroxytryptamine by KB-R7943, a Na(+)/Ca(2+) exchange inhibitor. Br J Pharmacol, 132: 1383-1388, 2001.
8. Kimura, J., Watano, T., Kawahara, M., Sakai, E., and Yatabe, J. Direction-independent block of bi-directional Na+/Ca2+ exchange current by KB-R7943 in guinea-pig cardiac myocytes. Br J Pharmacol, 128: 969-974, 1999.
9. Watano, T., Harada, Y., Harada, K., and Nishimura, N. Effect of Na+/Ca2+ exchange inhibitor, KB-R7943 on ouabain-induced arrhythmias in guinea-pigs. Br J Pharmacol, 127: 1846-1850, 1999.
10. Yang, H. T., Sakurai, K., Sugawara, H., Watanabe, T., Norota, I., and Endoh, M. Role of Na+/Ca2+ exchange in endothelin-1-induced increases in Ca2+ transient and contractility in rabbit ventricular myocytes: pharmacological analysis with KB-R7943. Br J Pharmacol, 126: 1785-1795, 1999.
