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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.
Sold for research purposes under agreement from GlaxoSmithKline
Compound Libraries for GSK 2193874
Technical Data for GSK 2193874
|Storage||Store at +4°C|
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|
|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|
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
3 Citations for GSK 2193874
Citations are publications that use Tocris products. Selected citations for GSK 2193874 include:
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
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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Literature in this Area
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Peripheral sensitization is the reduction in the threshold of excitability of sensory neurons that results in an augmented response to a given external stimulus. This poster outlines the excitatory and inhibitory signaling pathways involved in modulation of peripheral sensitization. The role of ion channels, GPCRs, neurotrophins, and cytokines in sensory neurons are also described.