Omecamtiv mecarbil (CK-1827452)
Molecular Weight(MW): 401.43
Omecamtiv mecarbil (CK-1827452) is a specific cardiac myosin activator and a clinical drug for left ventricular systolic heart failure. Phase 2.
Cited by 6 Publications
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Normal and Mutation human iPSC-CMs Structure when Treated with Omecamtiv Mecarbil. Human iPSC-CMs were plated on 100 kPa flat PDMS and grown for five days and left untreated, treated acutely on day 5, or treated continuously from the time of plating with the myosin activator Omecamtiv Mecarbil. iPSC-CMs were then fixed and stained for actin filaments (phalloidin, red) and nucleus (DAPI, blue). (a, c, e) Normal and (b, d, f) Mutation untreated, acutely treated, and continuously treated iPSC-CMs.
University of Illinois at Chicago 2014 Omecamtiv mecarbil (CK-1827452) purchased from Selleck.
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|Description||Omecamtiv mecarbil (CK-1827452) is a specific cardiac myosin activator and a clinical drug for left ventricular systolic heart failure. Phase 2.|
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||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. |
|In vitro||DMSO||80 mg/mL (199.28 mM)|
|Ethanol||6 mg/mL (14.94 mM)|
|In vivo||Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
1% DMSO+30% polyethylene glycol+1% Tween 80
For best results, use promptly after mixing.
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02929329||Recruiting||Heart Failure||Amgen|Cytokinetics|Servier||January 6 2017||Phase 3|
|NCT01786512||Completed||Modified Release Oral Formulation|Left Ventricular Systolic Dysfunction|Chronic Heart Failure|History of Chronic Heart Failure|Left Ventricular Ejection Fraction|Pharmacokinetics|Echocardiogram||Amgen|Cytokinetics||February 26 2013||Phase 2|
|NCT01300013||Completed||Heart Failure||Amgen|Cytokinetics||April 2011||Phase 2|
|NCT01077167||Withdrawn||Heart Failure||Amgen||July 2010||Phase 2|
|NCT00941681||Completed||Heart Failure||Cytokinetics||April 2009||Phase 2|
|NCT00748579||Terminated||Heart Failure||Cytokinetics||September 2008||Phase 2|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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Frequently Asked Questions
We would like to know the half-life of S2623, could you please provide some information?
In a press release from cytokinetics (http://www.cytokinetics.com/press_releases/release/pr_1133989715), the company claimed that CK-1827452 has a sufficiently long half-life to support oral dosing. In a later press release (http://www.cytokinetics.com/press_releases/release/pr_1213309188), cytokinetics updated clinical trail result and mentioned that the elimination half-life of CK-1827452 is 22 hours.