2. Membrane Transporter/Ion Channel
  3. Sodium Channel
  4. GS967

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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CAS 番号 : 1262618-39-2

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>無料サンプル (0.1 - 0.2 mg)   今すぐ申し込む  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 67 在庫あり
Solution
10 mM * 1 mL in DMSO USD 67 在庫あり
Solid
5 mg $61 在庫あり
10 mg $94 在庫あり
25 mg $188 在庫あり
50 mg $340 在庫あり
100 mg $540 在庫あり
200 mg $756 在庫あり
250 mg $860 在庫あり
500 mg $1200 在庫あり
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カスタマーレビュー

Based on 8 publication(s) in Google Scholar

Other Forms of GS967:

GS967 関連抗体

Top Publications Citing Use of Products

    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).

    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.

    Sodium Channel アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    Nav1.1 Nav1.2 Nav1.3 Nav1.4 Nav1.5 Nav1.6 Nav1.7 Nav1.8 Nav1.9

    • 生物活性

    • プロトコル

    • 純度とドキュメンテーション

    • 参考文献

    • カスタマーレビュー

    製品説明

    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.

    IC50 & Target

    IC50: 0.13 μM (late INa , ventricular myocytes )and 0.21 μM (late INa , isolated hearts)[1]
    Cellular Effect
    Cell Line Type Value Description References
    HEK293 IC50
    333 nM
    Compound: 2; GS-458967
    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 measured immediately after third compound addition by PatchXpress method
    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 measured immediately after third compound addition by PatchXpress method
    		[PMID: 27038498]
    体外実験

    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.

    GS967 関連抗体
    体内実験

    GS967 prevents and reverses proarrhythmic effects of the late INa enhancer ATX-II and the IKr inhibitor E-4031. GS967 significantly attenuates the proarrhythmic effects of methoxamine 1 clofilium and suppressed ischemia-induced arrhythmias[1]. GS967 causes a reduction of INaP in a frequency-dependent manner, consistent with use-dependent block (UDB). GS967 evokes more potent UDB of INaP (IC50=0.07 μM) than ranolazine (16 μM) and lidocaine (17 μM). GS967 is found to exert these same effects on a prototypical long QT syndromemutation (delKPQ)[2]. GS967 prevents ischemia-induced increases in alternans in the left atrium and left ventricle. GS967 reduces ischemia-induced increases in depolarization heterogeneity and repolarizationheterogeneity. GS967 does not alter heart rate, arterial blood pressure, PR and QT intervals, or QRS duration, but it mildly decreased contractility during ischemia, which was consistent with late INa inhibition[3].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    分子量

    347.22

    分子式

    C14H7F6N3O
    CAS 番号
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    FC(C1=NN=C2C=CC(C3=CC=C(OC(F)(F)F)C=C3)=CN21)(F)F
    輸送条件

    Room temperature in continental US; may vary elsewhere.
    保管条件
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    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)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.8800 mL 14.4001 mL 28.8002 mL
    5 mM 0.5760 mL 2.8800 mL 5.7600 mL
    10 mM 0.2880 mL 1.4400 mL 2.8800 mL
    View the 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.

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    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始）

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    体内:

    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.

    • Protocol 1

      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.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (7.20 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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    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).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    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.
    純度とドキュメンテーション
    参考文献
    動物実験
    [1][2]

    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) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    参考文献

    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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    GS967 Related Classifications

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
    × = ×
    C1   V1   C2   V2
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      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    GS9671262618-39-2GS 967GS-967Sodium ChannelNa channelsNa+ channelsInhibitorinhibitorinhibit

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    製品名:
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    製品番号:
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