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

GSK1016790A 

Cat. No.: HY-19608 Purity: 99.67%
Handling Instructions

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.

For research use only. We do not sell to patients.

GSK1016790A Chemical Structure

GSK1016790A Chemical Structure

CAS No. : 942206-85-1

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Customer Review

Based on 4 publication(s) in Google Scholar

Top Publications Citing Use of Products

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

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

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

    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.

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    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

     

    Ca2+

     

    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].

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

    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].

    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.
    SMILES

    O=C(C1=CC2=CC=CC=C2S1)N[[email protected]](C(N3CCN(C([[email protected]@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 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 33 mg/mL (50.33 mM)

    *"≥" 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
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 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

    • 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

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.08 mg/mL (3.17 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References

    Purity: 99.67%

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    Keywords:

    GSK1016790ATRP ChannelCalcium ChannelTransient receptor potential channelsCa2+ channelsCa channelstransientreceptorpotentialvanilloid4HEKhumanembryonickidneyInhibitorinhibitorinhibit

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    Product Name:
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    Cat. No.:
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