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530533 TRPV4 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).

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: GSK101, Transient Receptor Potential Vanilloid 4 Channel Agonist

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530533
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Overview

Replacement Information

Key Spec Table

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
      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
      Catalogue Number GTIN
      5305330001 04055977260854

      Documentation

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

      Title

      Safety Data Sheet (SDS) 

      TRPV4 Agonist, GSK1016790A - CAS 942206-85-1 - 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
      CAS number942206-85-1
      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.