Omecamtiv mecarbil (CK-1827452)
For research use only.
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.
Selleck's Omecamtiv mecarbil (CK-1827452) has been cited by 24 publications
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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.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
In vivo Formulation Calculator (Clear solution)
|Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)|
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|% DMSO % % Tween 80 % ddH2O|
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
Method for preparing in vivo formulation：Take μL DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH2O，mix and clarify.
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT04464525||Withdrawn||Drug: Omecamtiv mecarbil||Chronic Heart Failure With Reduced Ejection Fraction||Amgen||December 18 2020||Phase 3|
|NCT01786512||Completed||Drug: Omecamtiv Mecarbil|Drug: Placebo||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||Drug: Placebo|Drug: Omecamtiv mecarbil||Heart Failure||Amgen|Cytokinetics||April 2011||Phase 2|
|NCT01077167||Withdrawn||Drug: Omecamtiv mecarbil||Heart Failure||Amgen||July 2010||Phase 2|
|NCT00941681||Completed||Drug: CK-1827452||Heart Failure||Cytokinetics||April 2009||Phase 2|
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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.