Omecamtiv mecarbil - CAS 873697-71-3
Catalog number: B0084-307758
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C20H24FN5O3
Molecular Weight:
401.43
COA:
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Targets:
Myosin
Description:
Omecamtiv mecarbil is a cardiac-specific myosin activator with an EC50 of 0.6 μM.
Ordering Information
Catalog Number Size Price Stock Quantity
B0084-307758 25 mg $198 In stock
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Publication citing BOC Sciences Products
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Purity:
>98%
Synonyms:
CK-1827452
MSDS:
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InChIKey:
RFUBTTPMWSKEIW-UHFFFAOYSA-N
InChI:
InChI=1S/C20H24FN5O3/c1-14-6-7-16(12-22-14)23-19(27)24-17-5-3-4-15(18(17)21)13-25-8-10-26(11-9-25)20(28)29-2/h3-7,12H,8-11,13H2,1-2H3,(H2,23,24,27)
Canonical SMILES:
CC1=NC=C(C=C1)NC(=O)NC2=CC=CC(=C2F)CN3CCN(CC3)C(=O)OC
1.Omecamtiv mecarbil: a new cardiac myosin activator for the treatment of heart failure.
Liu LC1, Dorhout B1, van der Meer P1, Teerlink JR2, Voors AA1. Expert Opin Investig Drugs. 2016 Jan;25(1):117-27. doi: 10.1517/13543784.2016.1123248. Epub 2015 Dec 19.
INTRODUCTION: Current available inotropic agents increase cardiac contractility, but are associated with myocardial ischemia, arrhythmias, and mortality. A novel selective cardiac myosin activator, omecamtiv mecarbil (CK-1827452/ AMG-423) is a small molecule that activates the sarcomere proteins directly, resulting in prolonged systolic ejection time and increased cardiac contractility.
2.Relative bioavailability, food effect, and safety of the single-dose pharmacokinetics of omecamtiv mecarbil following administration of different modified-release formulations in healthy subjects.
Palaparthy R, Banfield C, Alvarez P, Yan L, Smith B, Johnson J, Monsalvo ML, Malik F. Int J Clin Pharmacol Ther. 2016 Mar;54(3):217-27. doi: 10.5414/CP202458.
OBJECTIVE: Omecamtiv mecarbil is a novel small molecule that directly activates cardiac myosin and increases cardiac contractility without increasing cardiac myocyte intracellular calcium. This study evaluated the relative bioavailability, food effect, and safety of several modified-release (MR) formulations of omecamtiv mecarbil.
3.Acute Treatment With Omecamtiv Mecarbil to Increase Contractility in Acute Heart Failure: The ATOMIC-AHF Study.
Teerlink JR1, Felker GM2, McMurray JJ3, Ponikowski P4, Metra M5, Filippatos GS6, Ezekowitz JA7, Dickstein K8, Cleland JG9, Kim JB10, Lei L10, Knusel B10, Wolff AA11, Malik FI11, Wasserman SM10; ATOMIC-AHF Investigators. J Am Coll Cardiol. 2016 Mar 29;67(12):1444-55. doi: 10.1016/j.jacc.2016.01.031.
BACKGROUND: Omecamtiv mecarbil (OM) is a selective cardiac myosin activator that increases myocardial function in healthy volunteers and in patients with chronic heart failure.
4.Manufacturing of [(14)C]-Labeled Drug Substance and Drug Product Utilized in Clinical Research: A Case Study of Omecamtiv Mecarbil.
Roberts SW1, Bezemer JM, Kennedy MT, Correll TL, Subramanian R, Walker SD. Curr Pharm Des. 2016;22(5):609-15.
This mini-review describes the Chemistry, Manufacturing and Control activities associated with the manufacture of [(14)C]-labeled drug substance and subsequent drug compounding activities to generate clinical trial material utilized in human absorption, distribution, metabolism, and excretion clinical studies. Due to the unstable nature and increased decomposition rates observed with [(14)C]-labeled compounds, the manufacture, testing, release, formulation, and regulatory filings are uniquely challenging. A case study of the cardiac myosin activator AMG 423 (omecamtiv mercarbil), utilized in a dual oral/intravenous infusion clinical study is presented.
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CAS 873697-71-3 Omecamtiv mecarbil

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