GSK1016790A

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.
Targets
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].

Protocol

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
Formula

C28H32Cl2N4O6S2

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

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID