GSK 2193874

Key Product Details

Product Description

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

Product Specifications for GSK 2193874

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Solubility

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 all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

2 1 Recalculate

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

Calculators

Background References

References are publications that support the biological activity of the product. See our Citations tab to view 38 publications citing the usage of this product.

• Cheung Discovery of GSK2193874: an orally active, potent, and selective blocker of transient receptor potential vanilloid 4. ACS Med.Chem.Lett. 2017 PMID: 28523109
• Thorneloe An orally active TRPV4 channel blocker prevents and resolves pulmonary edema induced by heart failure. Sci.Transl.Med. 2012 PMID: 23136043

Product Documents for GSK 2193874