| Identification | Back Directory | [Name]
Quinoline, 6-(3,6-dihydro-6-methyl-2-oxo-2H-1,3,4-thiadiazin-5-yl)-1-(3,4-dimethoxybenzoyl)-1,2,3,4-tetrahydro-, ( )- | [CAS]
147527-31-9 | [Synonyms]
Emd 57033
( )Emd 57033
(+)-EMD 57033
Quinoline, 6-(3,6-dihydro-6-methyl-2-oxo-2H-1,3,4-thiadiazin-5-yl)-1-(3,4-dimethoxybenzoyl)-1,2,3,4-tetrahydro-, ( )- | [Molecular Formula]
C22H23N3O4S | [MOL File]
147527-31-9.mol | [Molecular Weight]
425.501 |
| Chemical Properties | Back Directory | [density ]
1.36±0.1 g/cm3(Predicted) | [storage temp. ]
-20C | [solubility ]
DMSO: 50mg/mL | [form ]
Off-white solid | [pka]
10.54±0.60(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
(+)-EMD 57033 is a cardiac troponin C (cTnC) activator, is a dominant Ca2+ sensitizer. (+)-EMD 57033 binds the cardiac/slow skeletal troponin C isoform and exerts myocardial contractile promotion function[1]. | [Biological Activity]
Cell permeable: yes''Primary Target
myosin''Reversible: yes | [in vivo]
(+)-EMD 57033 (0.4 or 0.8 mg/kg/min; i.v.drip; over than 20 min) enhances contractility and achieves Ca2+ sensitization in intact failing hearts at substantial energetic savings and without compromise of diastolic function in dogs[4].
| Animal Model: | Mongrel dogs implanted with a micromanometer in left ventricle (LV) at the apex via lateral thoracotomy[4] | | Dosage: | 0.4 or 0.8 mg/kg/min | | Administration: | Intravenous drip; infused over 20 minutes | | Result: | Enhanced contractility at both doses, with similar changes in CON (conscious dogs) and HF (heart failure dogs) hearts.
Decreased the end-diastolic pressure (EDP) and lowered arterial load or preload at 0.8 mg/kg/min. |
| [References]
[1] 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 Jul 6;276(27):25456-66. DOI:10.1074/jbc.M102418200
[2] Ochala J, et al. EMD 57033 partially reverses ventilator-induced diaphragm muscle fibre calcium desensitisation. Pflugers Arch. 2010 Feb;459(3):475-83. DOI:10.1007/s00424-009-0744-1
[3] Hgashiyama A, et al. Effects of EMD 57033 on contraction and relaxation in isolated rabbit hearts. Circulation. 1995 Nov 15;92(10):3094-104. DOI:10.1161/01.cir.92.10.3094
[4] Senzaki H, et al. Improved mechanoenergetics and cardiac rest and reserve function of in vivo failing heart by calcium sensitizer EMD-57033. Circulation. 2000 Mar 7;101(9):1040-8. DOI:10.1161/01.cir.101.9.1040 |
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| Company Name: |
Merck KGaA
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| Tel: |
21-20338288 |
| Website: |
www.sigmaaldrich.cn |
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