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Chemical Structure : GS967
CAS No.: 1262618-39-2
Catalog No.: 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.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg (Free Sample) | $28 | In stock | |
| 10 mg | $88 | In stock | |
| 25 mg | $148 | In stock | |
| 50 mg | $228 | In stock | |
| 100 mg | Get quote |
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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.
| M.Wt | 347.2153 | |
| Formula | C14H7F6N3O | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
1,2,4-Triazolo[4,3-a]pyridine, 6-[4-(trifluoromethoxy)phenyl]-3-(trifluoromethyl)- |
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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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