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147527-31-9

147527-31-9 structure
147527-31-9 structure
  • Name: (+)-EMD 57033
  • Chemical Name: (+)-EMD 57033
  • CAS Number: 147527-31-9
  • Molecular Formula: C22H23N3O4S
  • Molecular Weight: 425.50
  • Catalog: Research Areas Cardiovascular Disease
  • Create Date: 2022-10-11 08:39:39
  • Modify Date: 2024-01-14 19:47:03
  • (+)-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].
Name (+)-EMD 57033
Description (+)-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].
Related Catalog
Target

Cardiac troponin C (cTnC)[1]

In Vitro (+)-EMD 57033 (30 μM) recovers the activation and sensitivity of Ca2+ in pig single muscle fibres and reduces VIDD (ventilator-induced diaphragm muscle fibre dysfunction) of [2]. (+)-EMD 57033 (5.0-5.8 μM; 10-15 min) significantly increases the coronary blood flow and myocardial V̇o2 (O2 consumption) in both 100 bpm and 150 bpm heart rates of rabbit heart, with a [Ca2+]0 concentration-dependent manner ([Ca2+]0=1.0 or 2.5 mM)[3]. (+)-EMD 57033 (5.0-5.8 μM; 10-15 min) increases left ventricular (LV) end-diastolic pressure and prolongs relaxation[3].
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.

[2]. Ochala J, et al. EMD 57033 partially reverses ventilator-induced diaphragm muscle fibre calcium desensitisation. Pflugers Arch. 2010 Feb;459(3):475-83.

[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. 

[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. 

Molecular Formula C22H23N3O4S
Molecular Weight 425.50
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title: CAS No. 147527-31-9 | Chemsrc address: https://www.chemsrc.com/en/baike/1719987.html

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