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Submit ReviewGSK 2193874
Description: Potent and selective TRPV4 antagonist; orally active
Chemical Name: 3-([1,4'-Bipiperidin]-1'-ylmethyl)-7-bromo-N-(1-phenylcyclopropyl)-2-[3-(trifluoromethyl)phenyl]-4-quinolinecarboxamide
Purity: ≥98% (HPLC)
Biological Activity for GSK 2193874
GSK 2193874 is a 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 for GSK 2193874
GSK 2193874 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for GSK 2193874
| M. Wt | 691.62 |
| Formula | C37H38BrF3N4O |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for GSK 2193874
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 34.58 | 50 with gentle warming |
Preparing Stock Solutions for GSK 2193874
The following data is based on the product molecular weight 691.62. 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 |
|---|---|---|---|
| 0.5 mM | 2.89 mL | 14.46 mL | 28.92 mL |
| 2.5 mM | 0.58 mL | 2.89 mL | 5.78 mL |
| 5 mM | 0.29 mL | 1.45 mL | 2.89 mL |
| 25 mM | 0.06 mL | 0.29 mL | 0.58 mL |
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Product Datasheets for GSK 2193874
References for GSK 2193874
References are publications that support the biological activity of the product.
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
If you know of a relevant reference for GSK 2193874, please let us know.
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Keywords: GSK 2193874, GSK 2193874 supplier, GSK2193874, potent, selectiveTRPV4, inhibitors, antagonists, orally, active, transient, receptors, potential, vanilloids, channels, myocardial, infarction, pulmonary, oedema, edema, inhibits, TRPV, 5106, Tocris Bioscience
9 Citations for GSK 2193874
Citations are publications that use Tocris products. Selected citations for GSK 2193874 include:
Sachio et al (2021) Resident cardiac macrophages mediate adaptive myocardial remodeling. Immunity 54 2072-2088.e7 PMID: 34320366
Brant E et al (2021) Endothelial pannexin 1-TRPV4 channel signaling lowers pulmonary arterial pressure in mice. Elife 10 PMID: 34490843
Yen-Lin et al (2021) Impaired TRPV4-eNOS signaling in trabecular meshwork elevates intraocular pressure in glaucoma. Proc Natl Acad Sci U S A 118 PMID: 33853948
Miriam et al (2021) Evaluating methods and protocols of ferritin-based magnetogenetics. iScience 24 103094 PMID: 34622149
Chen et al (2016) Transient Receptor Potential Vanilloid 4 Ion Channel Functions as a Pruriceptor in Epidermal Keratinocytes to Evoke Histaminergic Itch. J Biol Chem 291 10252 PMID: 26961876
Xu et al (2016) A novel TRPV4-specific agonist inhibits monocyte adhesion and atherosclerosis. Oncotarget 7 37622 PMID: 27191895
Girija et al (2022) Mechanical control of innate immune responses against viral infection revealed in a human lung alveolus chip. Nat Commun 13 1928 PMID: 35396513
Miriam et al (2020) Lipid Oxidation Induced by RF Waves and Mediated by Ferritin Iron Causes Activation of Ferritin-Tagged Ion Channels. Cell Rep 30 3250-3260.e7 PMID: 32160534
Neubert NCX1 Represents an Ionic Na+ Sensing Mechanism in Macrophages. PLoS Biol 18 PMID: 32569301
Do you know of a great paper that uses GSK 2193874 from Tocris? Please let us know.
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