GSK 1016790A

Key Product Details

Product Description

GSK 1016790A is a potent TRPV4 agonist; elicits Ca²⁺ influx in human and mouse TRPV4-expressing HEK cells (EC₅₀ values of 2.1 and 18 nM, respectively). Enhances insulin mRNA expression. Increases ERK1/2 phosphorylation and NO production. Exhibits no activity at TRPM8 and TRPA1 (20 μM) channels. Induces bladder overactivity in TRPV4^+/+ mice.

Product Specifications for GSK 1016790A

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Solubility

Preparing Stock Solutions for GSK 1016790A

The following data is based on the product molecular weight 655.61.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.53 mL	7.63 mL	15.25 mL
5 mM	0.31 mL	1.53 mL	3.05 mL
10 mM	0.15 mL	0.76 mL	1.53 mL
50 mM	0.03 mL	0.15 mL	0.31 mL

Calculators

Background References

References are publications that support the biological activity of the product. See our Citations tab to view 51 publications citing the usage of this product.

• Thorneloe N-((1S)-1-{[4-((2S)-2-{[(2,4-dichlorophenyl)sulfonyl]amino}-3-hydroxypropanoyl)-1-piperazinyl]carbonyl}-3-methylbutyl)-1-benzothiophene-2-carboxamide (GSK1016790A), a novel and potent transient receptor potential vanilloid 4 channel agonist induces urinary bladder contraction and hyperactivity: Part I. J.Pharmacol.Exp.Ther. 2008 PMID: 18499743
• Billert TRPV4 regulates insulin mRNA expression and INS-1E cell death via ERK1/2 and NO-dependent mechanisms. Cell Signal. 2017 PMID: 28359774

Product Documents for GSK 1016790A