500469 | RyR-Calstabin Interaction Stabilizer, S107 - Calbiochem

500469
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₁₁H₁₅NOS

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      5.00469.0001
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      Stocked 
      Discontinued
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      Available
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          Glass bottle 10 mg
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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
          FormOff-white solid
          Hill FormulaC₁₁H₁₅NOS
          Chemical formulaC₁₁H₁₅NOS
          Structure formula ImageStructure formula Image
          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

          Documentation

          SDS

          Title

          Safety Data Sheet (SDS) 

          References

          Reference overview
          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.
          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.

          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
          Chemical formulaC₁₁H₁₅NOS
          Structure formulaStructure formula
          Purity≥98% by HPLC
          SolubilityDMSO (100 mg/ml)
          Storage +2°C to +8°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
          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.