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Omecamtiv mecarbil

In stock
Catalog No.
A8349
Cardiac myosin activator
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$129.00
In stock
Evaluation Sample
$28.00
In stock
5mg
$119.00
In stock
10mg
$225.00
In stock
50mg
$679.00
In stock

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Background

Omecamtiv mecarbil (CK-1827452) is the first potent cardiac myosin activator that can specifically activate the cardiac myosin S1 domain but not other muscle myosins. In clinical trials, omecamtiv mecarbil has been considered as a promising therapeutic approach to treat systolic heart failure1.

Omecamtiv mecarbil accelerates the actin-dependent Pi release from cardiac myosin S1 domain, thus increases the rate of transition from weakly actin-bound state to strongly actin-bound state (EC50= 2.3 μM)1.

At the concentration of 200nM, omecamtiv mecarbil was reported to remarkably increase the contractility of adult rat cardiac myocytes without influencing calcium transient. In vivo, Omecamtiv mecarbil has been shown to improve cardiac function without changing myocardial oxygen consumption in both beagle dogs and Sprague-Dawley rats under isoflurane anesthesia1.

References:
1. Malik FI1, Hartman JJ, Elias KA, Morgan BP, Rodriguez H, Brejc K, Anderson RL, Sueoka SH, Lee KH, Finer JT, Sakowicz R, Baliga R, Cox DR, Garard M,Godinez G, Kawas R, Kraynack E, Lenzi D, Lu PP, Muci A, Niu C, Qian X, Pierce DW, Pokrovskii M, Suehiro I, Sylvester S, Tochimoto T, Valdez C, Wang W,Katori T, Kass DA, Shen YT, Vatner SF, Morgans DJ. Cardiac myosin activation: a potential therapeutic approach for systolic heart failure. Science. 2011 Mar 18;331(6023):1439-43.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt401.43
Cas No.873697-71-3
FormulaC20H24FN5O3
SynonymsCK-1827452; CK1827452
Solubility≥19.1mg/mL in DMSO
Chemical Namemethyl 4-[[2-fluoro-3-[(6-methylpyridin-3-yl)carbamoylamino]phenyl]methyl]piperazine-1-carboxylate
SDFDownload SDF
Canonical SMILESCC1=NC=C(C=C1)NC(=O)NC2=CC=CC(=C2F)CN3CCN(CC3)C(=O)OC
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Protocol

Cell experiment [1]:

Cell lines

Cardiac myocytes

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20 °C for several months.

Reaction Conditions

200 nM

Applications

Omecamtiv Mecarbil extended the duration of contraction without affecting the rates of contraction or relaxation. In addition, Omecamtiv Mecarbil also increased myocyte contraction in the presence of a β-adrenergic blocker, Carvedilol.

Animal experiment [1]:

Animal models

Conscious and heart failure dogs

Dosage form

A bolus at 0.5 mg/kg, followed by infusion at 0.5 mg/kg per hr

Applications

In a conscious canine model, Omecamtiv Mecarbil improved left ventricular systolic function. In heart failure dogs, Omecamtiv Mecarbil significantly increased stroke volume and cardiac output.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Malik FI1, Hartman JJ, Elias KA, Morgan BP, Rodriguez H, Brejc K, Anderson RL, Sueoka SH, Lee KH, Finer JT, Sakowicz R, Baliga R, Cox DR, Garard M,Godinez G, Kawas R, Kraynack E, Lenzi D, Lu PP, Muci A, Niu C, Qian X, Pierce DW, Pokrovskii M, Suehiro I, Sylvester S, Tochimoto T, Valdez C, Wang W,Katori T, Kass DA, Shen YT, Vatner SF, Morgans DJ. Cardiac myosin activation: a potential therapeutic approach for systolic heart failure. Science. 2011 Mar 18;331(6023):1439-43.

Biological Activity

Description Omecamtiv mecarbil (CK-1827452) is a specific activator of cardiac myosin activator and a clinical drug for left ventricular systolic heart failure.
Targets ATPase          
IC50            

Quality Control

Quality Control & MSDS

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Chemical structure

Omecamtiv mecarbil

Related Biological Data

Omecamtiv