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Omecamtiv mecarbil (CK-1827452)
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产品介绍
产品介绍
产品信息
抗原名称
Myosin ATPase
商品描述
Omecamtivmecarbil (CK-1827452) is a specific cardiac myosinactivator and a clinical drug for left ventricular systolic heart failure.
分子量
401.43
纯度
>98%
可溶性
DMSO 80 mg/mL (199.28 mM)
Ethanol 6 mg/mL (14.94 mM)
Ethanol 6 mg/mL (14.94 mM)
外观
Powder
In vitro(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.
In vivo(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.
背景
别名
CK-1827452, CK1827452,CK 1827452
分子式
C20H24FN5O3
CAS号
873697-71-3
制备和贮存
保存方式
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
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