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: 873697-71-3

Selleck's Omecamtiv mecarbil (CK-1827452) has been cited by 29 Publications

2 Customer Reviews

Purity & Quality Control

Batch: Purity: 99.66%
99.66

Other ATPase Products

Related compound libraries

Choose Selective ATPase Inhibitors

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NCT04464525 Withdrawn Chronic Heart Failure With Reduced Ejection Fraction Cytokinetics December 18 2020 Phase 3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NCT01077167 Withdrawn Heart Failure Cytokinetics July 2010 Phase 2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 lnformation & 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


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

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.

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

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.

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.

ATPase Signaling Pathway Map

Tags: buy Omecamtiv mecarbil (CK-1827452) | Omecamtiv mecarbil (CK-1827452) supplier | purchase Omecamtiv mecarbil (CK-1827452) | Omecamtiv mecarbil (CK-1827452) cost | Omecamtiv mecarbil (CK-1827452) manufacturer | order Omecamtiv mecarbil (CK-1827452) | Omecamtiv mecarbil (CK-1827452) distributor