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

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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GSK1016790A Chemical Structure

GSK1016790A Chemical Structure

CAS No. : 942206-85-1

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Customer Review

Based on 23 publication(s) in Google Scholar

GSK1016790A Related Antibodies

Top Publications Citing Use of Products

    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.

    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.

    View All TRP Channel Isoform Specific Products:

    View All Isoforms
    TRPC TRPM TRPV TRPA TRPML

    View All Calcium Channel Isoform Specific Products:

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

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    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]
    In Vitro

    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 Related Antibodies
    In Vivo

    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.
    Molecular Weight

    655.61

    Formula

    C28H32Cl2N4O6S2
    CAS No.
    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
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    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
    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)

    Mass
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    Concentration
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    Volume
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    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    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

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    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.
    Purity & Documentation

    Purity: 99.79%

    SDS (393 KB)

    COA (249 KB) LCMS (275 KB)

    Handling Instructions (2659 KB)
    References

    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

    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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