GSK 1016790A
Tocris Bioscience, part of Bio-Techne | Catalog # 6433
Potent TRPV4 agonist; active in vivo
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
Molecular Weight
655.61
Formula
C28H32Cl2N4O6S2
Storage
Store at -20°C
Purity
≥97% (HPLC)
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
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.
Solubility
| 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 all 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 |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
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 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 Specific Notices for GSK 1016790A
For research use only
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