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CK 1827452

(CAS No:873697-71-3)
Omecamtiv mecarbil (CK-1827452) is a specific cardiac myosin activator and a clinical drug for left ventricular systolic heart failure. Phase 2.
CAS No:873697-71-3
Molecular Weight(MW):401.43
Purity:99.00%
Specification:500MG;1G;5G;10G;50G;100G
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QC Documents
 COA  MSDS  HPLC  NMR
ChemicalInfomation
CAS No: 873697-71-3
Molecular formula(MF) C20H24FN5O3
Molecular Weight(MW): 401.43
Alias
Solubility
In vitro DMSO 80 mg/mL (199.28 mM)
Ethanol 6 mg/mL (14.94 mM)
Water <1 mg/mL
In vivo 1% DMSO+30% polyethylene glycol+1% Tween 80 30 mg/mL
Biological Activity
Description Omecamtiv mecarbil (CK-1827452) is a specific cardiac myosin activator and a clinical drug for left ventricular systolic heart failure. Phase 2.
Targets
Myosin ATPase [1]
In vitro

In vitro, Omecamtiv mecarbil selectively activates cardiac myosin by increasing the myosin ATPase rate. [1] 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. [1]

In vivo Omecamtiv mecarbil significantly increases fractional shortening starting at 0.4 mM plasma concentrations in SD rats, sham animals and in rats with heart failure. [1] 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. [2]