616522 TRPV4 Antagonist III, GSK205 - Calbiochem

616522
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616522-10MG
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      Glass bottle 10 mg
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      Description
      Overview

      This product has been discontinued.



      A pyridinylthiazolamine compound that is shown to inhibit TRPV4-mediated Ca2+ influx induced by 1 µM 4α-PDD (Cat. No. 524394) or Hypo-osmotic stress in primary porcine articular chondrocytes (10 µM GSK205 pretreatment). Also reported to effectively block Ca2+ mobilization induced by 100 nM TRPV4 agonist GSK101 in murine 3T3-F442A adipocytes in vitro and improve glucose tolerance (1 g/kg glucose via i.p.) in high fat diet-induced obese mice (10 mg GSK205/kg/12 h; i.p.) in vivo.

      Please note that the molecular weight for this compound is batch-specific due to variable water content.

      Catalogue Number616522
      Brand Family Calbiochem®
      SynonymsN-(4-(2-(Benzyl(methyl)amino)ethyl)phenyl)-5-(pyridin-3-yl)thiazol-2-amine, HBr
      References
      ReferencesYe, L., et al. 2012. Cell 151, 96.
      Phan, M.N., et al. 2009. Arthritis Rheum. 60, 3028.
      Product Information
      FormOrange powder
      Hill FormulaC₂₄H₂₄N₄S • HBr
      Chemical formulaC₂₄H₂₄N₄S • HBr
      Hygroscopic Hygroscopic
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetTRPV4 channel
      Purity≥97% 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 Ambient Temperature Only
      Toxicity Standard Handling
      Storage +2°C to +8°C
      Protect from Light Protect from light
      Hygroscopic Hygroscopic
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      References

      Reference overview
      Ye, L., et al. 2012. Cell 151, 96.
      Phan, M.N., et al. 2009. Arthritis Rheum. 60, 3028.
      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.

      Revision27-September-2013 JSW
      SynonymsN-(4-(2-(Benzyl(methyl)amino)ethyl)phenyl)-5-(pyridin-3-yl)thiazol-2-amine, HBr
      DescriptionA pyridinylthiazolamine compound that is shown to inhibit TRPV4-mediated Ca2+ influx induced by 1 µM 4α-PDD (Cat. No. 524394; cell population with intracellular Ca2+ fluctuation = 18% and 41% above control, respectively, with or without 10 µM GSK205 pretreatment) or Hypo-osmotic stress (280 mOsm; cell population with intracellular Ca2+ fluctuation = 2% and 83% above iso-osmotic control, respectively, with or without 10 µM GSK205 pretreatment) in primary porcine articular chondrocytes. Also reported to effectively block Ca2+ mobilization induced by 100 nM TRPV4 agonist GSK101 (by 100% with 10 µM GSK205) in murine 3T3-F442A adipocytes in vitro and improve glucose tolerance (1 g/kg glucose via i.p.) in high fat diet-induced obese mice ([peak plasma glucose] = 283 mg/dL vs. 346 mg/dL with or without 7 d 10 mg GSK205/kg/12 h i.p. treatment) in vivo.
      FormOrange powder
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₂₄H₂₄N₄S • HBr
      Structure formulaStructure formula
      Purity≥97% by HPLC
      SolubilityDMSO (100 mg/ml) or H₂O (100 mg/ml)
      Storage +2°C to +8°C
      Hygroscopic
      Protect from light
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
      Toxicity Standard Handling
      ReferencesYe, L., et al. 2012. Cell 151, 96.
      Phan, M.N., et al. 2009. Arthritis Rheum. 60, 3028.