GSK 1016790A

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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)
Citations (3)

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
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 Data for GSK 1016790A

Solvent Max Conc. mg/mL Max Conc. mM
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.

Select a batch to recalculate based on the batch molecular weight:
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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Product Datasheets for GSK 1016790A

Certificate of Analysis / Product Datasheet
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References for GSK 1016790A

References are publications that support the biological activity of the product.

Billert et al (2017) TRPV4 regulates insulin mRNA expression and INS-1E cell death via ERK1/2 and NO-dependent mechanisms. Cell Signal. 35 242 PMID: 28359774

Thorneloe et al (2008) 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. 326 432 PMID: 18499743

If you know of a relevant reference for GSK 1016790A, please let us know.

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Keywords: GSK 1016790A, GSK 1016790A supplier, GSK1016790A, trpv4, transient, receptor, potential, channels, potent, selective, agonists, agonism, activators, vanilloid, TRPV, 6433, Tocris Bioscience

3 Citations for GSK 1016790A

Citations are publications that use Tocris products. Selected citations for GSK 1016790A include:

Kwon et al (2023) TRPV4-Rho GTPase complex structures reveal mechanisms of gating and disease. Nat Commun 14 3732 PMID: 37353484

Stefanie et al (2020) The Effects of the Anti-aging Protein Klotho on Mucociliary Clearance. Front Med (Lausanne) 6 339 PMID: 32039219

Brant E et al (2021) Endothelial pannexin 1-TRPV4 channel signaling lowers pulmonary arterial pressure in mice. Elife 10 PMID: 34490843

Do you know of a great paper that uses GSK 1016790A from Tocris? Please let us know.

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