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

Directly and selectively binds to the troponin complex in fast skeletal muscle (Kd = 40 nM) and sensitizes it to calcium.

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Synonymes: 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, Tirasemtiv, CK-357

Primary Target: troponin complex
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531230
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CAS #Empirical Formula
1005491-05-3C₁₂H₁₄N₄O

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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®
      Synonyms6-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, Tirasemtiv, CK-357
      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
      Quality LevelMQ100
      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
      Global Trade Item Number
      Référence GTIN
      5.31230.0001 04055977242690

      Documentation

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

      Titre

      Fiche de données de sécurité des matériaux (FDS) 

      Références bibliographiques

      Aperçu de la référence bibliographique
      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.
      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.

      Revision31-July-2014 JSW
      Synonyms6-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, Tirasemtiv, CK-357
      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 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 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.