531230 Troponin Activator, CK-2017357 - CAS 1005491-05-3 - Calbiochem

531230
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₁₂H₁₄N₄O 1005491-05-3

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      5.31230.0001
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          Glass bottle 10 mg
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          Description
          OverviewAn orally bioavailable, non-toxic imidazopyrazinol compound that directly and selectively binds to the troponin complex in fast skeletal muscle (Kd = 40 nM) and sensitizes it to calcium. Its binding site is believed to be between two or more troponin subunits. Exhibits very modest affinity for slow skeletal muscle troponin (Kd = 3.8 µM) and has no measurable affinity for cardiac muscle troponin. Effectively stimulates myosin ATPase activity in fast skeletal muscle (EC50 = 390 nM), but has significantly reduced effect on mixed fiber type (EC50 = 770 nM in bovine rectus abdominis muscle). Slows the first order rate constant for Ca2+ release by about 70% (from 14.7 s-1 to 4.0 s-1) and shifts the plot of myosin ATPase relationship to calcium leftwards in fast skeletal muscles without increasing the maximum recorded force or the shape of the curve. Shown to improve muscle function in a rodent model of neuromuscular disease where neural input is diminished.

          Please note that the molecular weight for this compound is batch-specific due to variable water content.
          Catalogue Number531230
          Brand Family Calbiochem®
          SynonymsTirasemtiv, CK-357, 6-Ethynyl-1-(3-pentanyl)-1H-imidazo[4,5-b]pyrazin-2-ol, 6-Ethynyl-1-(pentan-3-yl)-1H-imidazo[4,5-b]pyrazin-2-ol, Fast Skeletal Troponin Activator, CK2017357
          References
          ReferencesGordon, P., et al. 2013. Expert Opin. Phamacother. 14, 1907.
          Miciak, J.J., et al. 2013. Muscle Nerve. 48, 279.
          Russell, A.J., et al. 2012. Nat. Med. 18, 452.
          Product Information
          CAS number1005491-05-3
          FormBeige powder
          Hill FormulaC₁₂H₁₄N₄O
          Chemical formulaC₁₂H₁₄N₄O
          ReversibleY
          Applications
          Biological Information
          Primary Targettroponin complex
          Purity≥98% by HPLC
          Physicochemical Information
          Cell permeableY
          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
          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

          Troponin Activator, CK-2017357 - CAS 1005491-05-3 - Calbiochem SDS

          Title

          Safety Data Sheet (SDS) 

          References

          Reference overview
          Gordon, P., et al. 2013. Expert Opin. Phamacother. 14, 1907.
          Miciak, J.J., et al. 2013. Muscle Nerve. 48, 279.
          Russell, A.J., et al. 2012. Nat. Med. 18, 452.
          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
          SynonymsTirasemtiv, CK-357, 6-Ethynyl-1-(3-pentanyl)-1H-imidazo[4,5-b]pyrazin-2-ol, 6-Ethynyl-1-(pentan-3-yl)-1H-imidazo[4,5-b]pyrazin-2-ol, Fast Skeletal Troponin Activator, CK2017357
          DescriptionAn orally bioavailable, non-toxic imidazopyrazinol compound that directly and selectively binds to the troponin complex in fast skeletal muscle (Kd = 40 nM) and sensitizes it to calcium. Its binding site is believed to be between two or more troponin subunits. Exhibits very modest affinity for slow skeletal muscle troponin (Kd = 3.8 µM) and has no measurable affinity for cardiac muscle troponin. Effectively stimulates myosin ATPase activity in fast skeletal muscle (EC50 = 390 nM), but has significantly reduced effect on mixed fiber type (EC50 = 770 nM in bovine rectus abdominis muscle). Slows the first order rate constant for Ca2+ release by about 70% (from 14.7 s-1 to 4.0 s-1) and shifts the plot of myosin ATPase relationship to calcium leftwards in fast skeletal muscles without increasing the maximum recorded force or the shape of the curve. Shown to improve muscle function in a rodent model of neuromuscular disease where neural input is diminished.
          FormBeige powder
          Intert gas (Yes/No) Packaged under inert gas
          CAS number1005491-05-3
          Chemical formulaC₁₂H₁₄N₄O
          Purity≥98% by HPLC
          SolubilityDMSO (25 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 6 months at -20°C).
          Toxicity Standard Handling
          ReferencesGordon, P., et al. 2013. Expert Opin. Phamacother. 14, 1907.
          Miciak, J.J., et al. 2013. Muscle Nerve. 48, 279.
          Russell, A.J., et al. 2012. Nat. Med. 18, 452.