GSK 1016790A

Name: GSK 1016790A
Brand: Tocris Bioscience
SKU: 6433

Tocris Bioscience, part of Bio-Techne | Catalog # 6433

Citations (44)

COA / SDS

Potent TRPV4 agonist; active in vivo

Key Product Details

Description:	Potent TRPV4 agonist; active in vivo
Chemical Name:	N-[(1S)-1-[[4-[(2S)-2-[[(2,4-Dichlorophenyl)sulfonyl]amino]-3-hydroxy-1-oxopropyl]-1-piperazinyl]carbonyl]-3-methylbutyl]benzo[b]thiophene-2-carboxamide
Purity:	≥97% (HPLC)
Molecular Weight:	655.61

View Full Technical Details for GSK 1016790A

Technical Data
Citations

Biological Activity for GSK 1016790A

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.

Compound Libraries for GSK 1016790A

GSK 1016790A is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for GSK 1016790A

M. Wt	655.61
Formula	C₂₈H₃₂Cl₂N₄O₆S₂
Storage	Store at -20°C
Purity	≥97% (HPLC)
CAS Number	942206-85-1
PubChem ID	23630211
InChi Key	IVYQPSHHYIAUFO-VXKWHMMOSA-N
Smiles	CC(C)C[C@H](NC(C1=CC2=CC=CC=C2S1)=O)C(N3CCN(CC3)C([C@H](CO)NS(=O)(C4=C(Cl)C=C(Cl)C=C4)=O)=O)=O

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

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for GSK 1016790A

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	65.56	100
	ethanol	65.56	100

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 will affect the solvent volumes required to prepare stock solutions.

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

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References for GSK 1016790A

References are publications that support the biological activity of the 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 urinar 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