For research use only.

Catalog No.S8107 Synonyms: GSK101

1 publication

GSK1016790A Chemical Structure

Molecular Weight(MW): 655.61

GSK1016790A (GSK101) is a novel, potent activator of TRPV4 (transient receptor potential vanilloid 4) with EC50 of 34nM in choroid plexus epithelial cells.

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Selleck's GSK1016790A has been cited by 1 publication

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Biological Activity

Description GSK1016790A (GSK101) is a novel, potent activator of TRPV4 (transient receptor potential vanilloid 4) with EC50 of 34nM in choroid plexus epithelial cells.
hTRPV4 [1]
(In HEK cells)
mTRPV4 [1]
(In HEK cells)
2.1 nM 18 nM
In vitro

GSK1016790A elicits Ca2+ influx in mouse and human TRPV4 expressing HEK cells (EC50 values of 18 and 2.1 nM, respectively), and evokes a dose-dependent activation of TRPV4 whole-cell currents at concentrations above 1 nM[1]. It stimulates TRPV4 in multiple cell types including endothelial cells, urinary smooth muscle cells, urothelial cells and HEK-293 cells over-expressing TRPV4. GSK1016790A specifically activates TRPV4 channels, leading to a rapid partial desensitization and downregulation of the channel expression on the plasma membrane[2].

In vivo GSK1016790A can produce marked decreases in systemic vascular resistance and pulmonary vascular resistance under high pulmonary vascular tone conditions[3]. The activation of TRPV4 by GSK1016780A leads to vasodilation, vascular leakage, and tissue hemorrhage[4].


Cell Research:[4]
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  • Cell lines: Choroid plexus epithelial cells
  • Concentrations: 10 nM
  • Incubation Time: 20 min
  • Method: CPECs are treated for 20 minutes with vehicle(DMSO), 10 nM GSK, or 10 nM GSK following the pretreatment with 1 mM HC. Then the cells are fixed and stained with Coomassie Brilliant Blue.
    (Only for Reference)
Animal Research:[3]
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  • Animal Models: Adult male Sprague-Dawley rats
  • Dosages: 2, 4, 6, 8, 10, and 12 μg/kg
  • Administration: Intravenous injection
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (152.52 mM)
Ethanol 100 mg/mL (152.52 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 655.61


CAS No. 942206-85-1
Storage powder
in solvent
Synonyms GSK101

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID