GS967
Based on 9 publication(s) in Google Scholar
GS967 (GS-458967) is a potent, and selective inhibitor of cardiac late sodium current (late INa ) with IC50 values of 0.13 and 0.21 μM for ventricular myocytes and isolated hearts, respectively.
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- Pureté: 99.55%
- CAS No.: 1262618-39-2
- Formule: C14H7F6N3O
- Masse moléculaire:347.22
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Publications Citing Use of MedChemExpress (MCE) GS967
More- Cell Stem Cell. 2020 Nov 5;27(5):813-821.e6. [Abstract]
- J Clin Invest. 2021 Nov 1;131(21):e142202. [Abstract]
- Circ Arrhythm Electrophysiol. 2017 Mar;10(3). pii: e004331. [Abstract]
- J Headache Pain. 2019 Nov 15;20(1):107. [Abstract]
- Br J Pharmacol. 2018 Dec;175(23):4325-4337. [Abstract]
- Cardiovasc Drugs Ther. 2018 Oct;32(5):413-425. [Abstract]
- J Cardiovasc Pharmacol. 2016 Oct;68(4):269-279. [Abstract]
- J Neurophysiol. 2019 Apr 1;121(4):1266-1278. [Abstract]
- medRxiv. 2026 May 21.
Customer Validation & Images
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Cell Proliferation/Viability Assay
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WB
Activité biologique
IC50: 0.13 μM (late INa , ventricular myocytes )and 0.21 μM (late INa , isolated hearts)[1]
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Cell Line
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Type | Value | Description | References |
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| HEK293 | IC50 |
333 nM
Compound: 2; GS-458967
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Inhibition of 0.1 Hz stimulated human Nav1.5alpha expressed in HEK293 cells assessed as inhibition of late sodium current with 3 compound additions for 7 to 8 mins at holding potential -120 mV in presence of late sodium current activator tefluthrin/ATX2 m
Inhibition of 0.1 Hz stimulated human Nav1.5alpha expressed in HEK293 cells assessed as inhibition of late sodium current with 3 compound additions for 7 to 8 mins at holding potential -120 mV in presence of late sodium current activator tefluthrin/ATX2 m
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[PMID: 27038498] |
GS967 (10, 100, 300 nM) completely attenuates the effect of ATX-II (10 nM) to increase action potential duration (APD) and APD variability in ventricular myocytes, with an apparent IC50 value of ～10 nM and decreased the beat-to-beat variability of APD[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1262618-39-2
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Appearance Solid
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Masse moléculaire 347.22
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Formule C14H7F6N3O
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Color White to off-white
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SMILES
FC(C1=NN=C2C=CC(C3=CC=C(OC(F)(F)F)C=C3)=CN21)(F)F
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (9)
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Journal Impact Factor
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Most Recent
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Cell Stem Cell
Reengineering an Antiarrhythmic Drug Using Patient hiPSC Cardiomyocytes to Improve Therapeutic Potential and Reduce Toxicity. [Abstract]2020 Nov 5;27(5):813-821.e6. PMID: 32931730 -
J Clin Invest
Hyperexcitable interneurons trigger cortical spreading depression in an Scn1a migraine model. [Abstract]2021 Nov 1;131(21):e142202. PMID: 34546973 -
Circ Arrhythm Electrophysiol
2017 Mar;10(3). pii: e004331. PMID: 28314848
GS967 purchased from MedChemExpress. Usage Cited in: Circ Arrhythm Electrophysiol. 2017 Mar;10(3). pii: e004331. [Abstract]
Effects of ranolazine and GS-967 on susceptibility to induction of ventricular refibrillation and spontaneous termination of initial long duration ventricular fibrillation (LDVF).
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J Headache Pain
Late sodium current blocker GS967 inhibits persistent currents induced by familial hemiplegic migraine type 3 mutations of the SCN1A gene. [Abstract]2019 Nov 15;20(1):107. PMID: 31730442 -
Br J Pharmacol
The transient receptor potential melastatin 4 channel inhibitor 9-phenanthrol modulates cardiac sodium channel. [Abstract]2018 Dec;175(23):4325-4337. PMID: 30153324 -
Cardiovasc Drugs Ther
Effects of the Inhibition of Late Sodium Current by GS967 on Stretch-Induced Changes in Cardiac Electrophysiology. [Abstract]2018 Oct;32(5):413-425. PMID: 30173392 -
J Cardiovasc Pharmacol
Pre- and Delayed Treatments With Ranolazine Ameliorate Ventricular Arrhythmias and Nav1.5 Downregulation in Ischemic/Reperfused Rat Hearts. [Abstract]2016 Oct;68(4):269-279. PMID: 27228311
GS967 purchased from MedChemExpress. Usage Cited in: J Cardiovasc Pharmacol. 2016 Oct;68(4):269-279. [Abstract]
Expression of total Nav1.5 protein is determined by Western blotting and the intensity of the bands is quantified by densitometry.
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J Neurophysiol
Adrenergic agonist induces rhythmic firing in quiescent cardiac preganglionic neurons in nucleus ambiguous via activation of intrinsic membrane excitability. [Abstract]2019 Apr 1;121(4):1266-1278. PMID: 30699052 -
Solvant et solubilité
DMSO : 50 mg/mL (144.00 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (7.20 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocole
Rats: Ventricular tachycardia or fibrillation are induced either by local aconitine injection (50 μg) in the left ventricular muscle of adult male rats or by arterial perfusion of 0.1 mM hydrogen peroxide in aged male rats. The left ventricular epicardial surface of the isolated-perfused hearts is optically mapped using fluorescent voltage-sensitive dye, and microelectrode recordings of action potentials are made adjacent to the aconitine injection site. The suppressive and preventive effects of GS967 (1 μM) against EAD/DAD-mediated ventricular tachycardia or fibrillation are then determined[2].
Rabbits: To determine the effect of GS967 on the inducibility of TdP by clofilium in the presence of methoxamine, rabbits are first treated with either vehicle or GS967 (in randomized manner) given as a 60 μg/kg bolus, followed by a 16 μg/kg/min infusion that is maintained for the duration of an experiment. After 10 minutes, methoxamine is infused intravenously at 15 μg/kg/min, followed 10 minutes later by clofilium at 100 nmol/kg/min. The incidences of premature ventricular contractions (PVCs), ventricular tachycardia (VT; defined as three or more consecutive abnormal beats), and TdP are determined from the ECG recordings[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureté et documentation
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Fiche technique (279 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
[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. [Content Brief]
[2]. Wei X, et al. Pre- and Delayed Treatments With Ranolazine Ameliorate Ventricular Arrhythmias and Nav1.5 Downregulation in Ischemic/Reperfused Rat Hearts. J Cardiovasc Pharmacol. 2016 Oct;68(4):269-279. [Content Brief]
[3]. Potet F, et al. Use-Dependent Block of Human Cardiac Sodium Channels by GS967. Mol Pharmacol. 2016 Jul;90(1):52-60. [Content Brief]
[4]. 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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.8800 mL | 14.4001 mL | 28.8002 mL | 72.0005 mL |
| 5 mM | 0.5760 mL | 2.8800 mL | 5.7600 mL | 14.4001 mL | |
| 10 mM | 0.2880 mL | 1.4400 mL | 2.8800 mL | 7.2000 mL | |
| 15 mM | 0.1920 mL | 0.9600 mL | 1.9200 mL | 4.8000 mL | |
| 20 mM | 0.1440 mL | 0.7200 mL | 1.4400 mL | 3.6000 mL | |
| 25 mM | 0.1152 mL | 0.5760 mL | 1.1520 mL | 2.8800 mL | |
| 30 mM | 0.0960 mL | 0.4800 mL | 0.9600 mL | 2.4000 mL | |
| 40 mM | 0.0720 mL | 0.3600 mL | 0.7200 mL | 1.8000 mL | |
| 50 mM | 0.0576 mL | 0.2880 mL | 0.5760 mL | 1.4400 mL | |
| 60 mM | 0.0480 mL | 0.2400 mL | 0.4800 mL | 1.2000 mL | |
| 80 mM | 0.0360 mL | 0.1800 mL | 0.3600 mL | 0.9000 mL | |
| 100 mM | 0.0288 mL | 0.1440 mL | 0.2880 mL | 0.7200 mL |
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