4-[[2-氟-3-[N'-(6-甲基吡啶-3-基)脲基]苯基]甲基
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产品名称:4-[[2-氟-3-[N'-(6-甲基吡啶-3-基)脲基]苯基]甲基]哌嗪-1-羧酸甲酯CAS:873697-71-3别名：4-[[2-氟-3-[N'-(6-甲基吡啶-3-基)脲基]苯基]甲基]哌嗪-1-羧酸甲酯;OMECAMTIVMECARBIL(CK-1827452);CK1827452英文名：OMecaMtiv Mecarbil
- 生物活性Omecamtiv mecarbil (CK-1827452)是一种特异性的心肌肌球蛋白激动剂，是用于左心室收缩性心脏衰竭的临床药物。Phase 2。
- 体外研究In vitro, Omecamtiv mecarbil selectively activates cardiac myosin by increasing the myosin ATPase rate. In isolated cardiac myocytes, Omecamtiv mecarbil results in increase of myocyte contractility and overcomes of the myosin inhibitor BDM without increasing the calcium transient or inhibiting the PDE pathway.
- 体内研究Omecamtiv mecarbil significantly increases fractional shortening starting at 0.4 mM plasma concentrations in SD rats, sham animals and in rats with heart failure. In conscious dogs with myocardial infarction (MI-sHF), Omecamtiv mecarbil leads to a significant increase in wall thickening (25%), stroke volume (44%), cardiac output (22%) and left ventricular (LV) systolic ejection time (26%). In addition, Omecamtiv mecarbil also results in the decreases of some hemodynamic parameters including heart rate, mean left atrial pressure, and LV end-diastolic pressure. In conscious dogs with left ventricular hypertrophy (LVH-sHF), Omecamtiv mecarbil leads to similar and not statistically different effects on hemodynamic parameters.
