GSK1016790A, >=98% (HPLC)

Not available outside of the UK & Ireland.

Application

GSK1016790A has been used:to stimulate transient receptor potential vanilloid 4 (TRPV4)-mediated currents in Xenopus laevis oocytesto 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

Biochem/physiol Actions

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).

Features and Benefits

This compound was developed by GlaxoSmithKline. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

Packaging

10, 50 mg in glass bottle