Agoniste TRPV4 ; GSK1016790A 1 pc x 10 mg

Non disponible en dehors du Royaume-Uni et de l'Irlande

Biochem/physiol Actions

Primary TargetTRPV4

General description

A cell-permeable piperazine amide derivative that acts as a potent and selective agonist of Transient Receptor Potential Vanilloid 4 Channel (TRPV4) and enhances Ca2+ flux in a variety of human and mouse cells (EC₅₀ = 2.1 nM and 18 nM in human and mouse TRPV4 expressed in HEK293 cells, respectively). Generates greater [Ca2+]i transients in chrondocytes than hypoosmotic treatments. Shown to be about 300-fold more potent that 4-α-PDD in activating TRPV4 channels. Suggested to act by recruiting previously inactive channels, rather than through increasing elevation of basal activity. Does not affect TRPM8 and TRPA1 channels even at high concentrations (~20 µM).Please note that the molecular weight for this compound is batch-specific due to variable water content.

A cell-permeable piperazine amide derivative that acts as a potent and selective agonist of Transient Receptor Potential Vanilloid 4 Channel (TRPV4) and enhances Ca2+ flux in a variety of human and mouse cells (EC₅₀ = 2.1 nM and 18 nM in human and mouse TRPV4 expressed in HEK293 cells, respectively). Generates greater [Ca2+]i transients in chrondocytes than hypoosmotic treatments. Shown to be about 300-fold more potent that 4-α-PDD in activating TRPV4 channels. Suggested to act by recruiting previously inactive channels, rather than through increasing elevation of basal activity. Does not affect TRPM8 and TRPA1 channels even at high concentrations (~20 µM).

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

O'Conor, C.J., 2014. PNAS.111, 1316.Sullivan, M.N., et al. 2012. Mol. Pharmacol.82, 464.Jun, M., et al. 2011. PLoS One.6, e16713. Thorneloe, K. S., et al. 2008. J. Pharm. Exp. Ther.326,432.

Packaging

Packaged under inert gas

10 mg in Glass bottle

Warning

Toxicity: Standard Handling (A)