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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-Sodium Channel-GS967
GS967

Chemical Structure : GS967

CAS No.: 1262618-39-2

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GS967 (GS-967, GS-458967, GS458967)

货号: PC-43116Not For Human Use, Lab Use Only.

GS-458967 (GS967) is a potent, selective inhibitor of cardiac late sodium current (late INa), inhibits TX-II-induced late INa in ventricular myocytes and isolated hearts with IC50 of 0.13 and 0.21 uM, respectively.

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10 mg ￥880 In stock
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50 mg ￥2280 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

GS-458967 (GS967) is a potent, selective inhibitor of cardiac late sodium current (late INa, Nav1.5), inhibits TX-II-induced late INa in ventricular myocytes and isolated hearts with IC50 of 0.13 and 0.21 uM, respectively.
GS967 displays >76-fold selectivity over inhibition of IKr (IC50>10 uM).
GS967 prevents and reverses proarrhythmic effects of the late I(Na) enhancer ATX-II and the I(Kr) inhibitor E-4031 in isolated ventricular myocytes and hearts.
GS967 significantly attenuates the proarrhythmic effects of methoxamine+clofilium and suppresses ischemia-induced arrhythmias in vivo.

物理化学性质&存储条件

分子量 347.2153
分子式 C14H7F6N3O
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

1,2,4-Triazolo[4,3-a]pyridine, 6-[4-(trifluoromethoxy)phenyl]-3-(trifluoromethyl)-

参考文献

1. Koltun DO, et al. Bioorg Med Chem Lett. 2016 Jul 1;26(13):3202-3206.

2. Belardinelli L, et al. J Pharmacol Exp Ther. 2013 Jan;344(1):23-32.

3. Bonatti R, et al. Heart Rhythm. 2014 Oct;11(10):1827-35.

4. Bossu A, et al. Br J Pharmacol. 2018 Mar 27. doi: 10.1111/bph.14217.

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