530657 | Myosin ATPase Activator, EMD57003 - CAS 147527-31-9 - Calbiochem

530657
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      Overview

      Replacement Information

      Key Spec Table

      Empirical FormulaCAS #
      C₂₂H₂₃N₃O₄S147527-31-9

      Pricing & Availability

      Catalogue NumberAvailability Packaging Qty/Pack Price Quantity
      5.30657.0001
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          Glass bottle 10 mg
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          Description
          OverviewA cell-permeable, bioavailable positive optical isomer of the racemate EMD-53998 that binds to the allosteric pocket of myosin motor domain (KD = 7.3 µM) and stimulates actomyosin ATPase activity (AC50 = 7.0 µM for β-cardiac myosin and 15.1 µM for skeletal muscle myosin). Exerts a positive inotropic effects on cardiac muscle and enhances diastolic performance while reducing oxygen cost of contraction in a canine canine model of tachycardia-induced heart failure. Acts as a pharmacological chaperone to protect β-cardiac myosin against heat stress and thermal denaturation and can induce refolding and reactivation of heat-inactivated myosin ATPase.
          Catalogue Number530657
          Brand Family Calbiochem®
          Synonyms(+)-5-(1-(3,4-Dimethoxybenzoyl)-1,2,3,4-tetrahydroquinolin-6-yl)-6-methyl-3,6-dihydro-2H-1,3,4-thiadiazin-2-one, (+)-6-(3,6-Dihydro-6-methyl-2-oxo-2H-1,3,4-thiadiazin-5-yl)-1-(3,4-dimethoxybenzoyl)-1,2,3,4-tetrahydroquinoline, EMD-57033, Myosin Motor Activator
          References
          ReferencesRadke, M.B., et al. 2014. ELife 3, e01603.
          Senzaki, H., et al., 2000. Circulation 101, 1040.
          Gambassi, G., et al. 1993. Am. J. Physiol. 264, H728.
          Solaro, R.J., et al.1993. Circ. Res.73, 981.
          Product Information
          CAS number147527-31-9
          FormOff-white solid
          Hill FormulaC₂₂H₂₃N₃O₄S
          Chemical formulaC₂₂H₂₃N₃O₄S
          ReversibleY
          Applications
          Biological Information
          Primary Targetmyosin
          Purity≥97% 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 -20°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

          SDS

          Title

          Safety Data Sheet (SDS) 

          References

          Reference overview
          Radke, M.B., et al. 2014. ELife 3, e01603.
          Senzaki, H., et al., 2000. Circulation 101, 1040.
          Gambassi, G., et al. 1993. Am. J. Physiol. 264, H728.
          Solaro, R.J., et al.1993. Circ. Res.73, 981.
          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.

          Revision12-June-2014 JSW
          Synonyms(+)-5-(1-(3,4-Dimethoxybenzoyl)-1,2,3,4-tetrahydroquinolin-6-yl)-6-methyl-3,6-dihydro-2H-1,3,4-thiadiazin-2-one, (+)-6-(3,6-Dihydro-6-methyl-2-oxo-2H-1,3,4-thiadiazin-5-yl)-1-(3,4-dimethoxybenzoyl)-1,2,3,4-tetrahydroquinoline, EMD-57033, Myosin Motor Activator
          DescriptionThe cell-permeable (+) enantiomer of the racemic tetrahydroquinoline EMD-53998 is reported to enhance myosin motor function via an 1:1 allosteric interaction with motor N-terminal SH3-like βbarrel subdomain (KD = 7.3 & 23 µM, respectively, using 100 nM porcine β-cardiac myosin S1 & rabbit fast skeletal muscle heavy meromyosin/HMM), restoring the ATP-binding activity of misfolded moysin as well as enhancing both basal and actin-dependent ATPase activity of myosin preparations (AC50 in µM = 7.0/porcine β-cardiac myosin S1, 15.1/rabbit HMM, 25.8/amoeba Dictyostelium discoideum Dd myosin-2, and 35.4/Dd myosin-5b), while being ineffective toward fully denatured myosin or βbarrel subdomain-lacking Dd myosin-1B/-1C/-1D/-1E. Pro-hypertrophic effect of EMD 57033 is demonstrated in serum-free neonatal rat cardiomyocyte cultures in vitro under both normal and hyperthermia conditions (cell size enlargement by 60% at 37 °C and by 24% at 42 °C; 10 µM EMD 57033 for 24 hr) with a drastic decline in cellular atrial natriuretic peptide only under hyperthermia condition (% of 37 °C control ANP level = 47% vs. 140%, respectively, with or without 10 µM EMD 57033 for 24 h at 42 °C), while positive inotropic efficacy is reported in vivo (0.4 mg/kg/min for 20 min) in a canine model of tachycardia-induced heart failure. The (-) enantiomer EMD 57439 is a known PDE3 inhibitor with little potency toward myosin ATPase activity.
          FormOff-white solid
          Intert gas (Yes/No) Packaged under inert gas
          CAS number147527-31-9
          Chemical formulaC₂₂H₂₃N₃O₄S
          Purity≥97% by HPLC
          SolubilityDMSO (50 mg/ml)
          Storage -20°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
          ReferencesRadke, M.B., et al. 2014. ELife 3, e01603.
          Senzaki, H., et al., 2000. Circulation 101, 1040.
          Gambassi, G., et al. 1993. Am. J. Physiol. 264, H728.
          Solaro, R.J., et al.1993. Circ. Res.73, 981.