530533 TRPV4 Agonist, GSK1016790A - Calbiochem

530533
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₂₈H₃₂Cl₂N₄O₆S₂

      Pricing & Availability

      Catalog Number AvailabilityPackaging Qty/Pack Price Quantity
      5.30533.0001
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          Glass bottle 10 mg
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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
          FormWhite powder
          Hill FormulaC₂₈H₃₂Cl₂N₄O₆S₂
          Chemical formulaC₂₈H₃₂Cl₂N₄O₆S₂
          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

          Documentation

          TRPV4 Agonist, GSK1016790A - Calbiochem SDS

          Title

          Safety Data Sheet (SDS) 

          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 -20°C
          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.
          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.