产品
编 号:F691130
分子式:C22H23N3O4S
分子量:425.5
产品类型
结构图
CAS No: 147527-31-9
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产品详情
生物活性:
(+)-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.
体内研究:
(+)-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.Animal Model:Mongrel dogs implanted with a micromanometer in left ventricle (LV) at the apex via lateral thoracotomy
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.
体外研究:
(+)-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 .(+)-EMD 57033 (5.0-5.8 μM; 10-15 min) significantly increases the coronary blood flow and myocardial V?o2 (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).(+)-EMD 57033 (5.0-5.8 μM; 10-15 min) increases left ventricular?(LV) end-diastolic pressure and prolongs relaxation.