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KB-R7943 mesylate

CAS号

182004-65-5

分子式

C17H21N3O6S2

主要靶点

Na+/Ca2+ Exchanger|Autophagy

仅限科研使用

Cat No : CM05242

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Synonyms

KB-R 7943|KB-R 7943 Mesylate|KB-R-7943|KBR7943 mesylate|KB-R7943 Mesylate|KB R7943 mesylate|Na+ Exchanger|Na+/Ca2+ Exchanger|Na+Exchanger|Autophagy|Ca2+Exchanger|Ca2+ Exchanger

验证数据展示

  • CAS No.: 182004-65-5

    KB-R7943 mesylate
    CAS#: 182004-65-5

产品信息

CAS号 182004-65-5
分子式 C17H21N3O6S2
主要靶点 Na+/Ca2+ Exchanger|Autophagy
主要通路 离子通道|自噬
分子量 427.5
纯度 99.22%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
别名 KB-R 7943|KB-R 7943 Mesylate|KB-R-7943|KBR7943 mesylate|KB-R7943 Mesylate|KB R7943 mesylate|Na+ Exchanger|Na+/Ca2+ Exchanger|Na+Exchanger|Autophagy|Ca2+Exchanger|Ca2+ Exchanger

靶点活性

Na+, Ca2+ exchanger:5.7±2.1 μM

体外活性

KB-R7943抑制了NCX(rev)，其IC(50)值为5.7 ± 2.1 μM，阻断了NMDAR介导的离子流，并且以IC(50) = 13.4 ± 3.6 μM抑制了NMDA诱导的胞浆Ca(2+)增加，但加速了在谷氨酸处理的神经元中的钙失调和线粒体去极化。KB-R7943以Ca(2+)-独立的方式使线粒体去极化。NMDA受体的刺激导致与ATP合成耦合或未耦合的NAD(P)H氧化，这取决于浴液中Ca(2+)的存在。KB-R7943或罗藤宁在静息条件下增加了NAD(P)H自荧光，并在添加谷氨酸后抑制了NAD(P)H的氧化。KB-R7943以IC(50) = 11.4 ± 2.4 μM抑制了培养神经元的2,4-二硝基苯酚激活的呼吸。在分离的脑线粒体中，当线粒体氧化复合物I底物时，KB-R7943抑制了呼吸、使器官去极化并抑制了Ca(2+)摄取，但在提供琥珀酸（复合物II底物）时无效。

溶解度

DMSO:55 mg/mL (128.65 mM)

细胞实验

Fluorescence microscopy, electrophysiological patch-clamp techniques and cellular respirometry with Seahorse XF24 analyzer were used with cultured hippocampal neurons;?membrane potential imaging, respirometry and Ca(2+) flux measurements were made in isolated rat brain mitochondria[1].

参考文献

1.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.[J]. British Journal of Pharmacology, 2015, 162(1):255-270.
2.Barrientos G , Bose D D , Feng W , et al. 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[J]. Molecular Pharmacology, 2009, 76(3):560-568.

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