GSK 1016790A

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Cat.No. 6433 - GSK 1016790A | C28H32Cl2N4O6S2 | CAS No. 942206-85-1
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: ≥98% (HPLC)
Datasheet
Citations
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Literature

Biological Activity

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.

Technical Data

M. Wt 655.61
Formula C28H32Cl2N4O6S2
Storage Store at -20°C
Purity ≥98% (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 Data

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

Preparing Stock Solutions

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

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 cha J.Pharmacol.Exp.Ther. 326 432 PMID: 18499743


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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

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