GSK1016790A is a novel and potent transient receptor potential vanilloid 4 (TRPV4) agonist. It has been used to demonstrate a role for TRPV4 in regulating urinary bladder activity and endothelial control of vascular tone. It elicited Ca2+ influx in mouse and human TRPV4 expressing HEK cells with EC50 values of 18 and 2.1 nM, respectively. It also evoked a dose-dependent activation of TRPV4 whole-cell currents at concentrations above 1 nM, which is 300 fold more potent than 4a-PDD. It was developed by GlaxoSmithKline.
Products > Drug Discovery > Inhibitor | Products > Drug Discovery > Inhibitor | Cardiovascular and blood system | TRP Channel
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