Home Transmembrane Transporters ATPase activator Omecamtiv mecarbil (CK-1827452) For research use only.

Omecamtiv mecarbil (CK-1827452)

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

Omecamtiv mecarbil (CK-1827452) Chemical Structure

Omecamtiv mecarbil (CK-1827452) Chemical Structure

CAS No. 873697-71-3

Purity & Quality Control

Omecamtiv mecarbil (CK-1827452) Related Products

Signaling Pathway

ATPase Signaling Pathways

ATPase Signaling Pathway

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 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
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]
Animal Research Animal Models Sprague Dawley rats.
Dosages ≤1.2 mg/kg/hour
Administration Administered via i.v.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04464525 Withdrawn
Chronic Heart Failure With Reduced Ejection Fraction
Cytokinetics
 December 18 2020 Phase 3
NCT02601001 Completed
Healthy Volunteer
Cytokinetics
 November 13 2015 Phase 1
NCT01300013 Completed
Heart Failure
Cytokinetics
 April 2011 Phase 2
NCT01077167 Withdrawn
Heart Failure
Cytokinetics
 July 2010 Phase 2

Chemical Information & Solubility

Molecular Weight 401.43 Formula

C20H24FN5O3
CAS No. 873697-71-3 SDF Download Omecamtiv mecarbil (CK-1827452) SDF
Smiles CC1=NC=C(C=C1)NC(=O)NC2=CC=CC(=C2F)CN3CCN(CC3)C(=O)OC
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 80 mg/mL ( (199.28 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 6 mg/mL

Water : Insoluble


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In vivo
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Tech Support

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

Question 1:
We would like to know the half-life of S2623, could you please provide some information?

Answer:
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.

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