KB-R7943 Mesylate
英文名称: KB-R7943 Mesylate
型号:null    产品货号: IIC1051-0010MG
价格:请致电:010-57128832,18610462672
品牌: gene operation

 IIC1051 KB-R7943 Mesylate中文网页版)

KB-R7943 Mesylate>99%

【英文同义名】:KB-R7943; KB-R 7943

【中文同义名】:KB-R7943 甲磺酰酸盐

订购信息:(原装进口,常备现货)

 

产品名称

产品货号

目录价(元)

Gene Operation

KB-R7943 Mesylate

IIC1051-0010MG

10 mg

¥1,879.00

IIC1051-0050MG

50 mg

¥6,059.00

产品描述

KB-R7943甲磺酸盐(KB)是选择性的Na+/Ca2+ 交换器(NCX)抑制剂 (IC50 = 0.7 μM)[1],并抑制ouabain嗜张力性作用,因此,在麻醉豚鼠中用于诱导室性早搏(VPB)、室性心动过速(VT)、心室纤颤(VF)和心脏骤停(CA)需要的ouabain剂量增加,而且KB-R7943甲磺酸盐可以延长离体心房中ouabain 诱导的额外收缩的发作时间[2]KB-R7943甲磺酸盐还可以抑制K+依赖的Na+/Ca2+交换器(NCKX) [3]和线粒体Ca2+单向转运体(MCU) (IC50 = 5.5 μM) [4]。另外,KB-R7943甲磺酸盐抑制钠离子门控通路(SGC),并降低通路开放几率而不影响单通道振幅[5]

靶点

靶点

Reverse mode of Na+/Ca2+ exchanger(NCX)

IC50(半数有效浓度)

0.7 μM

化学特性

Cas No.: 182004-65-5

M. Wt.: 427.49

Formula: C16H17N3O3S·CH3SO3H

Purity: >99%

Synonym: KB-R7943; KB-R 7943

Chemical Name: 2-[2-[4-(4-Nitrobenzyloxy)phenyl]ethyl]isothiourea mesylate

Appearance: White crystalline solid to tan solid

Solubility: Soluble to 100 mM in DMSO

StorageStore at -20 ºC

储存液配制

储存液 (1 ml DMSO体系)

10mM

20mM

30mM

质量(mg)

4.2749

8.5498

12.8247

结构式

                        

使用浓度(仅作参考)

KB-R7943 Mesylate具体使用浓度请参考相关文献,并根据自身实验条件(如实验目的,细胞种类,培养特性等)进行摸索和优化。

参考文献

[1] Hoyt KR. et al. Reverse Na+/Ca2+ exchange contributes to glutamate-induced intracellular Ca2+ concentration increases in cultured rat forebrain neurons. Mol Pharmacol. 53(4):742-9(1998).

[2] Watano, T., et al. Effect of Na+/Ca2+ exchange inhibitor, KB-R7943 on ouabain-induced arrhythmias in guinea-pigs. Br. J. Pharmacol. 127: 1846-1850(1999).

[3] Su, Y.H., et al. A flagellar K+-dependent Na+/Ca2+ exchanger keeps Ca2+ low in sea urchin spermatozoa. PNAS 99(10): 6743-6748(2002).

[4] Santo-Domingo, J., et al. 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). 

[5] Pezier, A., et al. The Na+/Ca2+ Exchanger Inhibitor, KB-R7943, Blocks a Nonselective Cation Channel Implicated in Chemosensory Transduction. J Neurophysiol 101(3): 1151-1159 (2009).