Omecamtiv mecarbil (CK-1827452)

Omecamtiv mecarbil (CK-1827452)CAS号: 873697-71-3分子式: C20H24FN5O3分子量: 401.43描述纯度储存/保存方法别名外观可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)

产品描述
描述
Omecamtivmecarbil (CK-1827452) is a specific cardiac myosinactivator and a clinical drug for left ventricular systolic heart failure.
纯度
>98%
储存/保存方法
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
基本信息
别名
CK-1827452, CK1827452,CK 1827452
外观
Powder
可溶性/溶解性
DMSO 80 mg/mL (199.28 mM)

Ethanol 6 mg/mL (14.94 mM)

生物活性
靶点
Myosin ATPase
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.

分子结构图

Omecamtiv mecarbil (CK-1827452)