GS967 |
Catalog No.GC10830
One-Click Copy Product Info
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GS967 is a potent and selective inhibitor of late sodium current (late INa) in ventricular myocytes and isolated hearts with IC50 values of 0.13 and 0.21µM, respectively.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1262618-39-2
Sample solution is provided at 25 µL, 10mM.
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GS967 is a potent and selective inhibitor of late sodium current (late INa) in ventricular myocytes and isolated hearts with IC50 values of 0.13 and 0.21µM, respectively [1]. GS967 can induce a hyperpolarized shift of steady-state channel inactivation and slowe both recovery from fast inactivation and onset of slow inactivation[2]. GS967 has been widely used in various models to block cardiac sodium channels, exhibiting antiarrhythmic effects [3].
In vitro, GS967 treatment inhibited peak sodium current (INaP) with use-dependent block (UDB) in cardiomyocytes derived from pluripotent stem cells within 400milliseconds, with an IC50 value of 0.07μM[4].
In vivo, GS967 treatment via oral administration at a dose of 1.5mg/kg/day for 38 days significantly prolonged the survival rate of Scn1a+/− mice and reduced seizure frequency[5]. For two consecutive days, administering a daily dose of 1.5mg/kg/day of GS967 significantly reduced the seizure frequency in Scn2aQ54 mice and prevented the loss of pulmonary ganglion neurons[6]. Oral administration of 1mg/kg/day dose of GS967 for 5 consecutive weeks significantly reduced the left ventricular mass and lung edema of Dahl salt-sensitive (DSS) rats on a high-salt diet, without affecting blood pressure or left ventricular contractility[7].
References:
[1] Belardinelli L, Liu G, Smith-Maxwell C, et al. A novel, potent, and selective inhibitor of cardiac late sodium current suppresses experimental arrhythmias[J]. The Journal of pharmacology and experimental therapeutics, 2013, 344(1): 23-32.
[2] Baker E M, Thompson C H, Hawkins N A, et al. The novel sodium channel modulator GS‐458967 (GS 967) is an effective treatment in a mouse model of SCN 8A encephalopathy[J]. Epilepsia, 2018, 59(6): 1166-1176.
[3] Vos M A, Houtman M, Antoons G, et al. GS967, By Blocking the Late Sodium Current (INaL), Has Strong Action Potential–Stabilizing Properties in Isolated Remodeled Ventricular Canine Cells[J]. Heart Rhythm, 2013, 10(11): 1742.
[4] Potet F, Egecioglu D E, Burridge P W, et al. GS-967 and eleclazine block sodium channels in human induced pluripotent stem cell–derived cardiomyocytes[J]. Molecular pharmacology, 2020, 98(5): 540-547.
[5] Anderson L L, Hawkins N A, Thompson C H, et al. Unexpected efficacy of a novel sodium channel modulator in Dravet syndrome[J]. Scientific reports, 2017, 7(1): 1682.
[6] Anderson L L, Thompson C H, Hawkins N A, et al. Antiepileptic activity of preferential inhibitors of persistent sodium current[J]. Epilepsia, 2014, 55(8): 1274-1283.
[7] Chi L, Belardinelli L, Zeng A, et al. Inhibition of late Na+ current, a novel target to improve diastolic function and electrical abnormalities in Dahl salt-sensitive rats[J]. American Journal of Physiology-Heart and Circulatory Physiology, 2016, 310(10): H1313-H1320.
| Animal experiment [1]: | |
Animal models | Scn1a+/− mice |
Preparation Method | On the 18th day after birth (P18), the Scn1a+/− mice were weaned and then randomly assigned to the GS967 group or the control group. Mice in the GS967 treatment group were fed food containing GS967 (at a dose of 1.5mg/kg/day). The survival rate of the mice was monitored until 8 weeks of age. At 8 weeks of age, the GS967 treatment was stopped, and the survival rate of the mice was monitored until 12 weeks of age. |
Dosage form | 1.5mg/kg/day for 38 days; p.o. |
Applications | GS967 treatment improved the survival of Scn1a+/− mice. |
References: | |
| Cas No. | 1262618-39-2 | SDF | |
| Chemical Name | 6-(4-(trifluoromethoxy)phenyl)-3-(trifluoromethyl)-[1,2,4]triazolo[4,3-a]pyridine | ||
| Canonical SMILES | FC(F)(F)C1=NN=C2C=CC(C3=CC=C(OC(F)(F)F)C=C3)=CN21 | ||
| Formula | C14H7F6N3O | M.Wt | 347.22 |
| Solubility | ≥ 13.35mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.88 mL | 14.4001 mL | 28.8002 mL |
| 5 mM | 576 μL | 2.88 mL | 5.76 mL |
| 10 mM | 288 μL | 1.44 mL | 2.88 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 15 reference(s) in Google Scholar.)