GSK-1016790A
TRPV4 channel blocker / A novel and potent TRPV4 channel agonist. GSK1016790A induced Ca2+ influx in mouse and human TRPV4 expressing HEK cells (EC50 values of 18 and 2.1 nM, respectively), and evoked a dose-dependent activation of TRPV4 whole-cell currents at concentrations above 1 nM. It is 300-fold more potent than 4α-PDD and is a valuable tool for investigating the role of TRPV4 in physiological processes.
Biochemicals & reagents
942206-85-1
1) Thorneloe et al. (2008), N-((1S)-1-{[4-((2S)-2-{[(2,4-dichlorophenyl)sulfonyl]amino}-3-hydroxypropanoyl)-1-piperazinyl]carbonyl}-3-methylbutyl)-1-benzothiophene-2-carboxamide (GSK1016790A), a novel and potent transient receptor potential vanilloid 4 channel agonist induces urinary bladder contraction and hyperactivity: Part I; J. Pharmacol. Exp. Ther., 326 432
-20°C
TARGET: Ion channel -- PATHWAY: Cation channel