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GS967

CAS号

1262618-39-2

分子式

C14H7F6N3O

主要靶点

Sodium Channel

仅限科研使用

Cat No : CM06492

Print datasheet

Synonyms

inhibit|GS458967|GS-458967|GS967|GS-967|GS 967|GS 458967|Na+ channels|Na channels|Inhibitor|late?INa?,isolated hearts|late?INa?,ventricular myocytes|SodiumChannel|Sodium Channel

验证数据展示

  • CAS No.: 1262618-39-2

    GS967
    CAS#: 1262618-39-2

产品信息

CAS号 1262618-39-2
分子式 C14H7F6N3O
主要靶点 Sodium Channel
主要通路 离子通道
分子量 347.22
纯度 100%， 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 inhibit|GS458967|GS-458967|GS967|GS-967|GS 967|GS 458967|Na+ channels|Na channels|Inhibitor|late?INa?,isolated hearts|late?INa?,ventricular myocytes|SodiumChannel|Sodium Channel

靶点活性

Late INa:0.13 μM

体内活性

GS967能防止和逆转晚期INa增强剂ATX-II及IKr抑制剂E-4031的致心律失常效应，并显著减轻methoxamine 1 clofilium引起的致心律失常效应，抑制缺血引起的心律失常[1]。GS967以频率依赖的方式减少INaP，符合使用依赖性阻断(UDB)。GS967引发的INaP UDB(半抑制浓度IC50=0.07μM)比ranolazine(16μM)和lidocaine(17μM)更强。GS967对典型的长QT综合征突变（delKPQ）[2]也表现出相同效应。GS967能阻止缺血引起的左心房和左心室alternans增加，减少缺血引起的去极化异质性和复极化异质性增加。GS967不改变心率、动脉血压、PR间期和QT间期或QRS持续时间，但在缺血期间轻度降低了心脏收缩性，这与晚期INa抑制一致[3]。

体外活性

GS967（10、100、300纳摩尔）完全抑制了ATX-II（10纳摩尔）增加心室肌细胞动作电位持续时间（APD）及APD变异性的效果，表观IC50值约为10纳摩尔，且减少了APD的搏动间变异性[1]。

溶解度

DMSO:50 mg/mL (144 mM)

参考文献

1.Belardinelli L, et al. A novel, potent, and selective inhibitor of cardiac late sodium current suppresses experimental arrhythmias. J Pharmacol Exp Ther. 2013 Jan;344(1):23-32.
2.Potet F, et al. Use-Dependent Block of Human Cardiac Sodium Channels by GS967. Mol Pharmacol. 2016 Jul;90(1):52-60.
3.Bonatti R, et al. Selective late sodium current blockade with GS-458967 markedly reduces ischemia-induced atrial and ventricular repolarization alternans and ECG heterogeneity. Heart Rhythm. 2014 Oct;11(10):1827-35.

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