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

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CAS #Empirical Formula
942206-85-1C₂₈H₃₂Cl₂N₄O₆S₂

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      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
      Référence GTIN
      5.30533.0001 04055977260854