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530533 TRPV4 Agonist, GSK1016790A - Calbiochem

Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₂₈H₃₂Cl₂N₄O₆S₂

Products

Catalog NumberPackaging Qty/Pack
5.30533.0001 Glass bottle 10 mg
Description
OverviewA 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.
Catalogue Number530533
Brand Family Calbiochem®
SynonymsGSK101, Transient Receptor Potential Vanilloid 4 Channel Agonist
References
ReferencesOʹConor, 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.
Product Information
FormWhite powder
Hill FormulaC₂₈H₃₂Cl₂N₄O₆S₂
Chemical formulaC₂₈H₃₂Cl₂N₄O₆S₂
Quality LevelMQ100
Applications
Biological Information
Primary TargetTRPV4
Purity≥98% by HPLC
Physicochemical Information
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
Toxicity Standard Handling
Storage -20°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Catalog Number GTIN
5.30533.0001 04055977260854

Documentation

TRPV4 Agonist, GSK1016790A - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

TRPV4 Agonist, GSK1016790A - Calbiochem Certificates of Analysis

TitleLot 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.

Revision31-July-2014 JSW
SynonymsGSK101, Transient Receptor Potential Vanilloid 4 Channel Agonist
DescriptionA 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).
FormWhite powder
Intert gas (Yes/No) Packaged under inert gas
Chemical formulaC₂₈H₃₂Cl₂N₄O₆S₂
Purity≥98% by HPLC
SolubilityDMSO (50 mg/ml)
Storage Protect from light
-20°C
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity Standard Handling
ReferencesOʹConor, 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.