KB-R7943 (mesylate)
货号：
16352-5mg 基本售价：
658.0 元 规格：
5 mg
产品信息
概述| 货号 | 16352-5mg |
| 描述 | 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.1 It is much less potent at preventing extracellular sodium-dependent calcium efflux from intact cells (IC50 > 30 µM).1 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).2 KB-R7943 has also been shown to block transient receptor potential canonical channels, which are important mediators of calcium-dependent signal transduction.3 |
性能| 供应商 | Cayman |
| 应用文献 |
1.Iwamoto, T.,Watano, T. and Shigekawa, M. A novel isothiourea derivative selectively inhibits the reverse mode of Na+/Ca2+ exchange in cells expressing NCX1. The Journal of Biological Chemisty 271(37), 22391-22397 (1996).
2.Brustovetsky, T.,Brittain, M.K.,Sheets, P.L., et al. KB-R7943, an inhibitor of the reverse Na+/Ca2+ exchanger, blocks N-methyl-D-aspartate receptor and inhibits mitochondrial complex I. British Journal of Pharmacology 162(1), 255-270 (2011).
3.Wu, X.,Eder, P.,Chang, B., et al. TRPC channels are necessary mediators of pathologic cardiac hypertrophy. Proceedings of the National Academy of Sciences of the United States of America 107(15), 7000-7005 (2010).
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| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 427.5 |
| 分子式 | C16H17N3O3S • CH3SO3H |
| CAS号 | 182004-65-5 |
| 稳定性 | ≥ 2 years |
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