Omecamtiv mecarbil (CK-1827452)

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产品名称：Omecamtiv mecarbil (CK-1827452)

产品别名：见爱必信官网

英文别名：Omecamtiv mecarbil (CK-1827452)

靶点：Myosin

CAS：873697-71-3

纯度：>98%

外观：见爱必信官网

保存方法：store at -20℃ for one year（Powder）； in DMSO or others solvent store at 2-4℃ for two weeks, at -80℃ for six months.

描述：Omecamtivmecarbil (CK-1827452) is a specific cardiac myosinactivator and a clinical drug for left ventricular systolic heart failure.

溶解性：DMSO 80 mg/mL (199.28 mM)
Ethanol 6 mg/mL (14.94 mM)

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.

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