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500469 RyR-Calstabin Interaction Stabilizer, S107 - CAS 927871-76-9 - Calbiochem

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Synonymes: 7-methoxy-4-methyl-2,3,4,5-tetrahydrobenzo[f][1,4]thiazepine, Ryanodine Receptor Stabilizer, Rycal S107

Primary Target: RyR2
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500469
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Tableau de caractéristiques principal

CAS #Empirical Formula
927871-76-9C₁₁H₁₅NOS

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5.00469.0001
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      Description
      OverviewA cell-permeable, orally active benzothiazepine that effectively blocks leaky intracellular calcium release by preventing the dissociation/depletion of calstabin from the ryanodine receptor (RyR) complex due to receptor modifications, such as oxidation, S-nitrosylation, hyperphosphorylation, or mutation (complete blockage of 1 mM tetracaine-induced leakage in murine RyR2 S2808D+/+ myocytes at 1 µM). Shown to prevent stress-induced cognitive dysfunction by stabilizing RyR2-calstabin-2 (FKBP12.6) interaction in brain (75 mg/kg/day; p.o.) and maintain exercise capacity by stabilizing RyR1-calstabin-1 (FKBP12) interaction in skeletal muscle (2.5 µg/0.25µL/h/animal; s.c) in mice, as well as restore normal cardiac function (20 mg/kg/day; s.c) in mice with R2474S or S2808D RyR2 mutation in vivo.

      Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.
      Catalogue Number500469
      Brand Family Calbiochem®
      Synonyms7-methoxy-4-methyl-2,3,4,5-tetrahydrobenzo[f][1,4]thiazepine, Ryanodine Receptor Stabilizer, Rycal S107
      References
      ReferencesLiu, X., et al. 2012. Cell. 150, 1055.
      Shan, J., et al. 2010. J. Clin. Invest. 120, 4375.
      Bellinger, A. M., et al. 2008. Proc. Natl. Acad. Sci. USA 105, 2198.
      Lehnart, S.E., et al. 2008. J. Clin. Invest. 118, 2230.
      Product Information
      CAS number927871-76-9
      FormOff-white solid
      Hill FormulaC₁₁H₁₅NOS
      Chemical formulaC₁₁H₁₅NOS
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetRyR2
      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 +2°C to +8°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
      Référence GTIN
      5.00469.0001 04055977245547

      Documentation

      RyR-Calstabin Interaction Stabilizer, S107 - CAS 927871-76-9 - Calbiochem FDS

      Titre

      Fiche de données de sécurité des matériaux (FDS) 

      Références bibliographiques

      Aperçu de la référence bibliographique
      Liu, X., et al. 2012. Cell. 150, 1055.
      Shan, J., et al. 2010. J. Clin. Invest. 120, 4375.
      Bellinger, A. M., et al. 2008. Proc. Natl. Acad. Sci. USA 105, 2198.
      Lehnart, S.E., et al. 2008. J. Clin. Invest. 118, 2230.
      Fiche technique

      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.

      Revision14-June-2013 JSW
      Synonyms7-methoxy-4-methyl-2,3,4,5-tetrahydrobenzo[f][1,4]thiazepine, Ryanodine Receptor Stabilizer, Rycal S107
      DescriptionA cell-permeable, orally active benzothiazepine derivative that effectively blocks leaky intracellular calcium release by preventing the dissociation/depletion of calstabin from the ryanodine receptor (RyR) complex due to receptor modifications, such as oxidation, S-nitrosylation, PKA-mediated hyperphosphorylation, or mutation (complete blockage of 1 mM tetracaine-induced leakage in murine RyR2 S2808D+/+ myocytes at 1 µM). Oral administration in mice (75 mg/kg/day via drinking water) is shown to prevent stress-induced cognitive dysfunction by stabilizing RyR2-calstabin-2 (FKBP12.6) interaction in brain of stressed animals. Likewise, s.c. administration (2.5 µg/0.25 µL/h/animal; by s.c. via neck dorsal surface osmotic pump implant) is reported to maintain mice exercise capacity by stabilizing RyR1-calstabin-1 (FKBP12) interaction in skeletal muscle following intensive exercise regimes. Also demonstrated to exhibit in vivo efficacy in restoring normal cardiac function in mice with R2474S (5 mg/kg/h; by s.c. via osmotic pump) or S2808D (20 mg/kg/day; by s.c. via osmotic pump) RyR2 mutation.
      FormOff-white solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number927871-76-9
      Chemical formulaC₁₁H₁₅NOS
      Structure formulaStructure formula
      Purity≥98% by HPLC
      SolubilityDMSO (100 mg/ml)
      Storage Protect from light
      +2°C to +8°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
      ReferencesLiu, X., et al. 2012. Cell. 150, 1055.
      Shan, J., et al. 2010. J. Clin. Invest. 120, 4375.
      Bellinger, A. M., et al. 2008. Proc. Natl. Acad. Sci. USA 105, 2198.
      Lehnart, S.E., et al. 2008. J. Clin. Invest. 118, 2230.