GSK1016790A

GSK1016790A is a potent and selective small molecule agonist of the transient receptor potential cation channel subfamily V member 4 (**TRPV4**), developed by GSK. It serves as a pharmacological tool to probe TRPV4 function in vitro and in vivo. Mechanistically, GSK1016790A activates TRPV4 channels, leading to effects such as increased intracellular calcium signaling, modulation of ion transport, regulation of smooth muscle tone (notably in blood vessels, lymphatic system, bladder, and colon), and altered membrane trafficking of the channel. Experimentally, the compound has been shown to have pronounced vasodilator activity, to modulate vascular resistance, and to induce the release of lipid mediators like arachidonic acid derivatives in various preclinical systems. Its main use is as a research tool; its development for clinical use remains preclinical, and it is not an approved therapeutic agent[1][3][5][7][9][11][12].

Other names

TRPV4 agonistTRPV-4 agonistTRPV 4 agonistTransient receptor potential cation channel subfamily V member 4 agonist