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

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NCT04464525 Withdrawn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NCT01077167 Withdrawn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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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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