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EMD57033

Catalog No. T25372   CAS 147527-31-9
Synonyms: EMD-57033, (+)-EMD 57033, EMD 57033

EMD57033 is a cardiac troponin C (cTnC) activator, a dominant Ca2+ sensitizer, which functions by binding to cardiac/slow skeletal troponin C heterodimers to promote cardiac contraction.

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EMD57033 Chemical Structure
EMD57033, CAS 147527-31-9
Pack Size Availability Price/USD Quantity
1 mg In stock $ 350.00
5 mg In stock $ 828.00
10 mg In stock $ 1,130.00
25 mg In stock $ 1,590.00
50 mg In stock $ 1,980.00
100 mg In stock $ 2,500.00
500 mg In stock $ 4,900.00
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Purity: 99.41%
Purity: 97.56%
ee: 99.58%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description EMD57033 is a cardiac troponin C (cTnC) activator, a dominant Ca2+ sensitizer, which functions by binding to cardiac/slow skeletal troponin C heterodimers to promote cardiac contraction.
In vitro EMD57033 (5.0 to 5.8 mumol/L) enhances contractility and prolongs relaxation. Its effects are modulated by heart rate, [Ca2+]o, and contraction mode, with positive inotropic effects being more prominent for ejecting beats.[4]
In vivo EMD-57033 (0.4 mg. kg(-1). min(-1) for 20 minutes) selective Ca(2+) sensitization with minimal PDE3I in vivo is achieved, improving basal and rate-stimulated contractility and mechanoenergetics of HF without compromising diastolic function. Despite PDE3I activity at higher doses, energetic benefits persist.[5]
Synonyms EMD-57033, (+)-EMD 57033, EMD 57033
Molecular Weight 425.5
Formula C22H23N3O4S
CAS No. 147527-31-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 45.0 mg/mL (105.8 mM)

TargetMolReferences and Literature

1. Papadaki M, et al. Uncoupling of myofilament Ca2+ sensitivity from troponin I phosphorylation by mutations can be reversed by epigallocatechin-3-gallate. Cardiovasc Res. 2015 ; 108(1):99-110. 2. Ørstavik Ø, et al. The inotropic effect of the active metabolite of levosimendan, OR-1896, is mediated through inhibition of PDE3 in rat ventricular myocardium. PLoS One. 2015 ; 10(3):e0115547. 3. Vikhorev PG, et al. The dilated cardiomyopathy-causing mutation ACTC E361G in cardiac muscle myofibrils specifically abolishes modulation of Ca(2+) regulation by phosphorylation of troponin I. Biophys J. 2014 ; 107(10):2369-80. 4. Hgashiyama A, et al. Effects of EMD 57033 on contraction and relaxation in isolated rabbit hearts. Circulation. 1995 ; 92(10):3094-3104. 5. Senzaki H, et al. Improved mechanoenergetics and cardiac rest and reserve function of in vivo failing heart by calcium sensitizer EMD-57033. Circulation. 2000 ; 101(9):1040-1048. 6. Ochala J, et al. EMD 57033 partially reverses ventilator-induced diaphragm muscle fibre calcium desensitisation. Pflugers Arch. 2010 ; 459(3):475-483. 7. Wang X, et al. Structure of the C-domain of human cardiac troponin C in complex with the Ca2+ sensitizing drug EMD 57033. J Biol Chem. 2001 ; 276(27):25456-25466.

Related compound libraries

This product is contained In the following compound libraries:
Membrane Protein-targeted Compound Library Neuronal Signaling Compound Library Anti-Cancer Metabolism Compound Library Bioactive Compound Library Bioactive Compounds Library Max

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Keywords

EMD57033 147527-31-9 Membrane transporter/Ion channel Metabolism Carbonic Anhydrase Calcium Channel EMD-57033 (+)-EMD 57033 EMD 57033 inhibitor inhibit

 

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