2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. TRP Channel Calcium Channel
  4. GSK1016790A

GSK1016790A  (Synonyms: GSK101)

製品番号: HY-19608 純度: 99.93%
COA 取扱説明書 Technical Support

GSK1016790A is a potent and selective transient receptor potential vanilloid 4 (TRPV4) channel agonist. GSK1016790A can elicit Ca2+ influx and elevate intracellular Ca2+ in HEK cells.

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CAS 番号 : 942206-85-1

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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 120 在庫あり
Solution
10 mM * 1 mL in DMSO USD 120 在庫あり
Solid
5 mg $83 在庫あり
10 mg $143 在庫あり
25 mg $308 在庫あり
50 mg $545 在庫あり
100 mg $902 在庫あり
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カスタマーレビュー

Based on 38 publication(s) in Google Scholar

GSK1016790A 関連抗体

Top Publications Citing Use of Products

顧客検証

Cell Migration/Invasion Assay
Others
Flow Cytometry
WB
IF

    GSK1016790A purchased from MedChemExpress. Usage Cited in: Signal Transduct Target Ther. 2025 Nov 28;10(1):388.  [Abstract]

    HC067047 (100 nM, transient administration) blocked both GSK1016790A (80 nM,transient administration) -evoked inward and outward transmembrane currents in HUVEC cells.

    GSK1016790A purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2023 Jun 28;14(6):379.  [Abstract]

    MHCC-97H and HCC-LM3 cells were treated with 4 μM GSK1016790A or 8 μM HC067047 for 24 h. Transwell migration assay without Matrigel matrix was detected and the number of transmigrated cells were quantified. Scale bar: 200 μm.

    GSK1016790A purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2023 Jun 28;14(6):379.  [Abstract]

    GSK1016790A (2-8 μM, 24 h). The expression of cytoskeleton-related proteins was measured by western blot.

    GSK1016790A purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2023 Jun 28;14(6):379.  [Abstract]

    The MHCC-97H cells were stimulated with 16 μM GSK1016790A for a brief period of time, and the calcium ion fluorescence intensity was acquired by flow cytometry analysis.

    GSK1016790A purchased from MedChemExpress. Usage Cited in: Acs Biomater Sci Eng. 2019 Dec 9;5(12):6520-6529.  [Abstract]

    Protein levels of NFATc1 in nuclei of BMSCs cultured on various surfaces with or without GSK101 and RN-1734.

    GSK1016790A purchased from MedChemExpress. Usage Cited in: Acs Biomater Sci Eng. 2019 Dec 9;5(12):6520-6529.  [Abstract]

    Effects of TRPV4 on NFATc1 nuclear localization in BMSCs on MNTs. Micrographs stained for NFATc1 of BMSCs cultured for 7d on (A) PT, (B) PT with TRPV4 agonist (GSK101) , (C) TNT-30, (D)TNT-100, (E) TNT-100 with TRPV4 antagonist (RN-1734). Red fluorescence: NFATc1; Blue fluorescence: nucleus.

    TRP 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
    TRPA1 TRPC3 TRPC4 TRPC5 TRPC6 TRPC7 TRPM8 TRPM2 TRPM3 TRPM4 TRPM7 TRPML1 TRPML2 TRPML3 TRPV1 TRPV2 TRPV3 TRPV4 TRPV6

    Calcium 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
    N-type calcium channel L-type calcium channel P/Q-type calcium channel T-type calcium channel Calcium Channel

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    • 純度とドキュメンテーション

    • 参考文献

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    製品説明

    GSK1016790A is a potent and selective transient receptor potential vanilloid 4 (TRPV4) channel agonist. GSK1016790A can elicit Ca2+ influx and elevate intracellular Ca2+ in HEK cells[1][2].

    IC50 & Target[1][2]

    TRPV4

     

    Cellular Effect
    Cell Line Type Value Description References
    HEK293 EC50
    49 nM
    Compound: 1; GSK1016790A
    Agonist activity at recombinant human TRPV4 expressed in HEK293 cells assessed as increase in intracellular calcium level after 30 mins by Fura-2 AM/Pluronic F-127 probe based fluorescence assay
    Agonist activity at recombinant human TRPV4 expressed in HEK293 cells assessed as increase in intracellular calcium level after 30 mins by Fura-2 AM/Pluronic F-127 probe based fluorescence assay
    		[PMID: 30629441]
    体外実験

    GSK1016790A (0.1-1000 nM) elicits Ca2+ influx in mouse and human TRPV4-expressing human embryonic kidney (HEK) cells (EC50 values of 18 and 2.1 nM, respectively) and it evokes a dose-dependent activation of TRPV4 whole-cell currents at concentrations above 1 nM. GSK1016790A (100 nM) treatment elicits a rapid elevation of intracellular Ca2+ in a subset of neurons[2].

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

    GSK1016790A 関連抗体
    体内実験

    GSK1016790A (0.001-0.1 mg/kg; i.p.) produces a dose-dependent inhibitory effect on whole gut transit time in mice[2].
    GSK1016790A (0.1-1000 nM; pretreatment 10 min) significantly inhibits the electrical field stimulation (EFS)-induced twitch contractions in isolated mouse colon strips in a concentration-dependent manner[2].

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

    Animal Model: S100β-GFP and TRPV4 knockout (TRPV4-/-) mice[2]
    Dosage: 0.001, 0.01, 0.1 mg/kg
    Administration: IP; single dose
    Result: Produced a dose-dependent inhibitory effect on whole gut transit time in mice.
    Produced a dose-dependent and time-dependent inhibitory effect on colonic expulsion.
    分子量

    655.61

    分子式

    C28H32Cl2N4O6S2
    CAS 番号
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(C1=CC2=CC=CC=C2S1)N[C@H](C(N3CCN(C([C@@H](NS(=O)(C4=CC=C(Cl)C=C4Cl)=O)CO)=O)CC3)=O)CC(C)C
    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: 

    Methanol : 50 mg/mL (76.26 mM; Need ultrasonic)

    DMSO : ≥ 33 mg/mL (50.33 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.5253 mL 7.6265 mL 15.2530 mL
    5 mM 0.3051 mL 1.5253 mL 3.0506 mL
    10 mM 0.1525 mL 0.7626 mL 1.5253 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.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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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）

    C1

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    体積 （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 (3.81 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      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% (20% SBE-β-CD in Saline)

      Solubility: 2.5 mg/mL (3.81 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

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    g

    Dosing volume
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    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
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    % 
    +
    %
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    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    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

    純度: 99.93%

    COA (250 KB) HNMR (255 KB) RP-HPLC (246 KB) MS (240 KB)

    取扱説明書 (2659 KB)
    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 / Methanol 1 mM 1.5253 mL 7.6265 mL 15.2530 mL 38.1324 mL
    5 mM 0.3051 mL 1.5253 mL 3.0506 mL 7.6265 mL
    10 mM 0.1525 mL 0.7626 mL 1.5253 mL 3.8132 mL
    15 mM 0.1017 mL 0.5084 mL 1.0169 mL 2.5422 mL
    20 mM 0.0763 mL 0.3813 mL 0.7626 mL 1.9066 mL
    25 mM 0.0610 mL 0.3051 mL 0.6101 mL 1.5253 mL
    30 mM 0.0508 mL 0.2542 mL 0.5084 mL 1.2711 mL
    40 mM 0.0381 mL 0.1907 mL 0.3813 mL 0.9533 mL
    50 mM 0.0305 mL 0.1525 mL 0.3051 mL 0.7626 mL
    Methanol 60 mM 0.0254 mL 0.1271 mL 0.2542 mL 0.6355 mL
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    GSK1016790A Related Classifications

    • Molarity Calculator

    • Dilution Calculator

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    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    質量   濃度   体積   分子量 *
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    The dilution calculator equation

    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
    Help & FAQs
    • Do most proteins show cross-species activity?

      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:

    GSK1016790A942206-85-1TRP ChannelCalcium ChannelTransient receptor potential channelsCa2+ channelsCa channelstransientreceptorpotentialvanilloid4HEKhumanembryonickidneyInhibitorinhibitorinhibit

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    製品名:
    GSK1016790A
    製品番号:
    HY-19608
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