Home Transmembrane Transporters TRP Channel activator GSK1016790A For research use only.

GSK1016790A

Synonyms: GSK101

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

GSK1016790A Chemical Structure

GSK1016790A Chemical Structure

CAS: 942206-85-1

Selleck's GSK1016790A has been cited by 8 publications

Purity & Quality Control

Batch: Purity: 99.82%
99.82

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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
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].
Cell Research 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.
In Vivo
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].
Animal Research Animal Models Adult male Sprague-Dawley rats
Dosages 2, 4, 6, 8, 10, and 12 μg/kg
Administration Intravenous injection

Chemical Information & Solubility

Molecular Weight 655.61 Formula

C28H32Cl2N4O6S2
CAS No. 942206-85-1 SDF Download GSK1016790A SDF
Smiles CC(C)CC(C(=O)N1CCN(CC1)C(=O)C(CO)NS(=O)(=O)C2=C(C=C(C=C2)Cl)Cl)NC(=O)C3=CC4=CC=CC=C4S3
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (152.52 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 66 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

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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