Omecamtiv mecarbil (CK-1827452)

Catalog No.S2623

Omecamtiv mecarbil (CK-1827452) Chemical Structure

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.

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1 Customer Review

  • 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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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]

Protocol

Animal Research
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  • Animal Models: Sprague Dawley rats.
  • Formulation: Omecamtiv mecarbil is dissolved in DMSO and then diluted in water.
  • Dosages: ≤1.2 mg/kg/hour
  • Administration: Administered via i.v.
    (Only for Reference)

Solubility (25°C)

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

* 1 mg/ml means slightly soluble or insoluble.
* 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.

Chemical Information

Molecular Weight 401.43
Formula

C20H24FN5O3

CAS No. 873697-71-3
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02695420 Recruiting Heart Failure With Reduced Ejection Fraction Amgen April 2016 Phase 2
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 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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID