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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10 mM * 1  mL in DMSO USD 121 In-stock
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10 mg USD 144 In-stock
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25 mg USD 300 In-stock
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50 mg USD 540 In-stock
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100 mg USD 900 In-stock
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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 Nov.

    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 Nov.

    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].

    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].

    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.

    942206-85-1

    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)

    H2O : < 0.1 mg/mL (insoluble)

    *"≥" 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: ≥ 2.5 mg/mL (3.81 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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