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48-602MAG
Buffer Detection Kit for Magnetic Beads
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530533
Sigma-AldrichTRPV4 Agonist, GSK1016790A - CAS 942206-85-1 - Calbiochem
A cell-permeable, potent, selective agonist of TRPV4 channel. Enhances Ca2+ flux in a variety of human and mouse cells (EC₅₀ = 2.1 nM for human TRPV4).
More>>A cell-permeable, potent, selective agonist of TRPV4 channel. Enhances Ca2+ flux in a variety of human and mouse cells (EC₅₀ = 2.1 nM for human TRPV4). Less<<
MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.
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Description
Overview
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.
TRPV4 Agonist, GSK1016790A - CAS 942206-85-1 - Calbiochem Certificates of Analysis
Title
Lot Number
530533
References
Reference overview
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.
Data Sheet
Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.
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).
Form
White powder
Intert gas (Yes/No)
Packaged under inert gas
CAS number
942206-85-1
Chemical formula
C₂₈H₃₂Cl₂N₄O₆S₂
Purity
≥98% by HPLC
Solubility
DMSO (50 mg/ml)
Storage
Protect from light -20°C
Do Not Freeze
Ok to freeze
Special Instructions
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity
Standard Handling
References
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.
