|[4-[(4-硝基苄基)氧代]苯基乙基]异硫脲甲磺酸盐|CsnPharm

CAS No.: 182004-65-5

KB-R7943 mesylate/S-[4-[(4-硝基苄基)氧代]苯乙基]异硫脲甲磺酸盐 Catalog No. CSN12367

Synonyms: KB-R7943 (mesylate);KB R7943

KB-R7943 Mesylate is a potent and selective inhibitor used to reverse mode of the Na+/Ca2+ exchanger with IC50 value of 0.7 μM. It also inhibits the mitochondrial Ca2+ uniporter with IC50 value of 5.5 μM.

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生物活性

描述KB-R7943 mesylate is a widely used inhibitor of the reverse Na+/Ca2+ exchanger (NCXrev) with IC50 of 5.7±2.1 µM. KB-R7943 mesylate induces cancer cell death via activating the JNK pathway and blocking autophagic flux. KB-R7943 mesylate blocks NMDAR-mediated ion currents, and inhibits NMDA-induced increase in cytosolic Ca2+ with IC50=13.4±3.6 µM but accelerates calcium deregulation and mitochondrial depolarization in glutamate-treated neurons. KB-R7943 depolarizes mitochondria in a Ca2+-independent manner. KB-R7943 inhibits 2,4-dinitrophenol-stimulated respiration of cultured neurons with IC50=11.4±2.4 µM. In addition to NCXrev, KB-R7943 dose-dependently and reversibly blocked ion currents elicited by NMDA. KB-R7943 dose-dependently inhibits NMDA-induced increases in [Ca2+]c with IC50=13.4±3.6 µM confirming the inhibition of NMDA receptors observed in electrophysiological experiments^[3]. wtRyR1-HEK 293 pretreated with KB-R7943 (10 μM, 10 min) dissolved in the bulk perfusion exhibited significantly attenuated responses to caffeine. In this regard, KB-R7943 produced more pronounced inhibition of caffeine-induced Ca2+ release elicited by 1 mM compared with 0.5 and 0.75 mM (60 versus 58 versus 37%, p<0.05, respectively)^[4]. KB-R7943 inhibits both IhERG and native IKr rapidly on membrane depolarization with IC50 values of ~89 and ~120 nM, respectively, for current tails at −40 mV following depolarizing voltage commands to +20 mV. IhERG inhibition by KB-R7943 exhibits both time- and voltage-dependence but shows no preference for inactivated over activated channels^[5]. In fish cardiomyocytes IKATP was blocked by KB-R7943 with an IC50 value of 3.14×10(-7) M, while in mammalian cells IC50 was 2.8×10(-6) M (P<0.05). 10(-5) M KB-R7943 inhibited CCCP-induced IKATP by 99.9±0.13% and 97.5±1.2% in crucian carp and mouse ventricular myocytes, respectively^[6].
参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.3392 mL
- 11.6960 mL
- 23.3921 mL
- 5 mM
- 0.4678 mL
- 2.3392 mL
- 4.6784 mL
- 10 mM
- 0.2339 mL
- 1.1696 mL
- 2.3392 mL

技术信息

CAS号

182004-65-5

储存条件

粉末: Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C17H21N3O6S2

运输

蓝冰

分子量

427.50

别名

KB-R7943 (mesylate);KB R7943

溶解度

DMSO	100.0 mg/mL (233.9 mM)
Water	insoluble

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KB-R7943 mesylate/S-[4-[(4-硝基苄基)氧代]苯乙基]异硫脲甲磺酸盐 Catalog No. CSN12367

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