Biological Activity
Potent and selective TRPV4 antagonist (IC50 values are 2 and 40 nM for rat and human receptors, respectively); inhibits Ca2+ influx through TRPV4 channels. Prevents and reverses pulmonary edema after myocardial infarction in vivo models. Selective over a panel of ~200 human receptors, channels and enzymes. Orally active.
Licensing Information
Sold for research purposes under agreement from GlaxoSmithKline
Compound Libraries
GSK 2193874 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 691.62 |
| Formula | C37H38BrF3N4O |
| Storage | Store at +4°C |
| CAS Number | 1336960-13-4 |
| PubChem ID | 53464483 |
| InChI Key | UIVOZBSCHXCGPS-UHFFFAOYSA-N |
| Smiles | O=C(NC6(CC6)C5=CC=CC=C5)C2=C(CN4CCC(N7CCCCC7)CC4)C(C3=CC(C(F)(F)F)=CC=C3)=NC1=CC(Br)=CC=C12 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| 1eq. HCl | 13.83 | 20 | |
| DMSO | 34.58 | 50 |
Preparing Stock Solutions
The following data is based on the product molecular weight 691.62. Batch specific molecular weights may vary from batch to batch due to solvent 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 | 1.45 mL | 7.23 mL | 14.46 mL |
| 5 mM | 0.29 mL | 1.45 mL | 2.89 mL |
| 10 mM | 0.14 mL | 0.72 mL | 1.45 mL |
| 50 mM | 0.03 mL | 0.14 mL | 0.29 mL |
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References
References are publications that support the products' biological activity.
Thorneloe et al (2012) An orally active TRPV4 channel blocker prevents and resolves pulmonary edema induced by heart failure. Sci.Transl.Med. 4 159 PMID: 23136043
Cheung et al (2017) Discovery of GSK2193874: an orally active, potent, and selective blocker of transient receptor potential vanilloid 4. ACS Med.Chem.Lett. 8 549 PMID: 28523109
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