TRPV4 AGONIST GSK1016790A (C15-1305-015)

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).

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.

Biochem/physiol Actions

Primary Target
TRPV4

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Other Notes

OʹConor, 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.

Legal Information

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

Molecular Weight: 655.61. Empirical Formula: C₂₈H₃₂Cl₂N₄O₆S₂. Assay: ≥. 98% (HPLC). Quality Level: 100. form: powder. manufacturer/tradename: Calbiochem^®. . storage condition: OK to freeze, protect from light. color: white. solubility: DMSO: 50 . mg/mL. storage temp.: −. 20°C. SMILES string: CC(C)CC(C(: O)N1CCN(CC1)C(: O)C(CO)NS(: O)(: O)C2: C(C: C(C: C2)Cl)Cl)NC(: O)C3: CC4: CC: CC: C4S3. Storage Class Code: 11 - Combustible Solids. WGK: WGK 1. Flash Point(F): Not applicable. Flash Point(C): Not applicable.