Omecamtiv mecarbil (CK-1827452) 873697-71-3

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Molecular Weight:

401.43 Omecamtiv mecarbil (CK-1827452) is a specific cardiac myosin activator and a clinical drug for left ventricular systolic heart failure. Phase 2.

Biological Activity

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.


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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Product Categories : Transmembrane Transporters > ATPase Inhibitor