942206-85-1

GSK-1016790A (942206-85-1) is a novel and potent TRPV4 channel activator. GSK-1016790A 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.

GSK 1016790A is a transient receptor potential vanilloid 4 (TRPV4) agonist.

GSK1016790A has been used:

• to stimulate transient receptor potential vanilloid 4 (TRPV4)-mediated currents in Xenopus laevis oocytes
• to stimulate cells in Ca²⁺ level measurement in human retinal capillary endothelial cells (HRCECs)
• to study the role of TRPV4 channels in brain injury after intracerebral hemorrhage (ICH)
• to trigger the opening of TRPV4 channels in bovine nucleus pulposus cells or Hanks′ Balanced Salt Solution

ChEBI: GSK1016790A is a tertiary carboxamide that is piperazine in which one of the amino groups has undergone condensation with the carboxy group of N-[(2,4-dichlorophenyl)sulfonyl]-L-serine, while the other has undergone condensation with the carboxy group of N-(1-benzothiophen-2-ylcarbonyl)-L-leucine. It is a cell-permeable, potent and selective agonist of the TRPV4 (transient receptor potential vanilloid 4) channel. It has a role as a TRPV4 agonist. It is a member of 1-benzothiophenes, a N-acylpiperazine, a sulfonamide, a dichlorobenzene, a tertiary carboxamide and an aromatic primary alcohol.

GSK1016790A is a novel and potent TRPV4 channel agonist. The TRPV4 (transient receptor potential vanilloid 4) member of the TRP superfamily has been implicated in numerous physiological processes. GSK1016790A elicited 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 4a-PDD (Cat. No. P8014).

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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