1336960-13-4

GSK 2193874 is an orally active, potent and selective TRPV4 antagonist.

GSK2193874 has been used as a transient receptor potential vanilloid 4 (TRPV4) antagonist:

• to study its effects on GSK101-induced colon contractions in mice
• to study its effects on murine compact bone-derived osteoblasts(CB-OB)
• to study its effects on lung injury post-lipopolysaccharide (LPS) in mice

GSK2193874 is a very potent, specific antagonist of TRPV4 ion channels (IC50 = 50 nM). Lung edema caused by high pulmonary venous pressure (PVP) is driven by TRPV4 activity. GSK2193874 blocks TRPV4-mediated calcium influx in cells expressing native and recombinant TRPV4, and inhibits vascular permeability and lung edema in isolated rodent and canine lungs subjected to high PVP. The compound also resolves pulmonary edema in murine myocardial infarction model.

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