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530533 TRPV4 Agonist, GSK1016790A - CAS 942206-85-1 - Calbiochem

Overview

Key Spec Table

CAS #Empirical Formula
942206-85-1C₂₈H₃₂Cl₂N₄O₆S₂

Products

Catalogue NumberPackaging Qty/Pack
5305330001 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
CAS number942206-85-1
FormWhite powder
Hill FormulaC₂₈H₃₂Cl₂N₄O₆S₂
Chemical formulaC₂₈H₃₂Cl₂N₄O₆S₂
Quality LevelMQ100
Biological Information
Primary TargetTRPV4
Purity≥98% by HPLC
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
Global Trade Item Number
Catalogue Number GTIN
5305330001 04055977260854