Omecamtiv mecarbil (CK-1827452)

Catalog No.S2623

For research use only.

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

CAS No. 873697-71-3

Selleck's Omecamtiv mecarbil (CK-1827452) has been cited by 25 publications

Purity & Quality Control

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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 (from reference)

Animal Research:[1]
  • Animal Models: Sprague Dawley rats.
  • Dosages: ≤1.2 mg/kg/hour
  • Administration: Administered via i.v.

Solubility (25°C)

In vitro

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.

30 mg/mL

Chemical Information

Molecular Weight 401.43
Formula

C20H24FN5O3

CAS No. 873697-71-3
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=NC=C(C=C1)NC(=O)NC2=CC=CC(=C2F)CN3CCN(CC3)C(=O)OC

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

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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 Cytokinetics December 18 2020 Phase 3
NCT02601001 Completed Drug: Omecamtiv mecarbil|Drug: Placebo Healthy Volunteer Cytokinetics November 13 2015 Phase 1
NCT01300013 Completed Drug: Placebo|Drug: Omecamtiv mecarbil Heart Failure Cytokinetics April 2011 Phase 2
NCT01077167 Withdrawn Drug: Omecamtiv mecarbil Heart Failure Cytokinetics July 2010 Phase 2

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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.

Handling Instructions

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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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