Omecamtiv mecarbil (CK1827452)

Alias: CK1827452; CK 1827452; CK1827452; Omecamtiv mecarbil.
Cat No.:V0063 Purity: ≥98%
Omecamtiv mecarbil (also known as CK-1827452) is a specific/selective cardiac myosin activator and a clinical drug for left ventricular systolic heart failure.
Omecamtiv mecarbil (CK1827452) Chemical Structure CAS No.: 873697-71-3
Product category: Myosin
This product is for research use only, not for human use. We do not sell to patients.
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Omecamtiv mecarbil (also known as CK-1827452) is a specific/selective cardiac myosin activator and a clinical drug for left ventricular systolic heart failure. Omecamtiv mecarbil is clinically investigated for its role in the treatment of left ventricular systolic heart failure. It specifically targets and activates myocardial ATPase and improves energy utilization. Omecamtiv Mecarbil improves systolic function by increasing the systolic ejection duration/stroke volume, without consuming more ATP energy, oxygen or altering intracellular calcium levels causing an overall improvement in cardiac efficiency.

Biological Activity I Assay Protocols (From Reference)
ln Vitro
Omecamtiv mecarbil (10 μM) significantly lowers the actin concentration at which ATPase is half-maximal (KATPase) by 30 times and the maximal ATPase (kcat) by 4.5 times. The concentration-dependent evaluation of the actin-activated ATPase inhibition mediated by omecamtiv mecarbil yields the EC50 value of 0.52 ± 0.10 μM. The total actin affinity is unchanged by omecamtiv mecarbil. Slow product release is achieved with omecamtiv mecarbil, which traps a population of myosin heads in a weak actin affinity condition. In the in vitro motility assay, omecamtiv mecarbil can reduce the actin sliding velocity by more than 100 times[3].
ln Vivo
Among Sprague, omecamtiv mecarbil (100-1000 ng/mL) exhibits concentration-dependent increases in FS.Model of Dawley rats. In both rats (Sprague-Dawley) and dogs (Beagle), omecamtiv mecarbil has good PK characteristics, with clearances of 22 and 7.2 mL /min/kg, volumes of 3.5 and 3.6 L/kg, and bioavailabilities (F%) of 100 and 80%, respectively[1]. Omecamtiv mecarbil does not alter the force generation at maximal Ca2+ activation (pCa 4.5) in any of the groups, nor does it alter the phosphorylation status of myofilament proteins in both WT and KO hearts, as demonstrated by the lack of significant differences between pre and post Omecamtiv mecarbil samples within WT and KO groups. The cardiac myofilaments' reactivity to Ca2+ is enhanced by omecamtiv mecarbil at submaximal Ca2+-activations[2].
Animal Protocol
Dissolved in DMSO and then diluted in water; ≤1.2 mg/kg/hour; i.v. injection.
Sprague Dawley rats.
References
[1]. Morgan BP, et al. Discovery of omecamtiv mecarbil the first, selective, small molecule activator of cardiac Myosin. ACS Med Chem Lett. 2010 Aug 20;1(9):472-7.
[2]. Mamidi R, et al. Molecular effects of the myosin activator omecamtiv mecarbil on contractile properties of skinned myocardium lacking cardiac myosin binding protein-C. J Mol Cell Cardiol. 2015 Aug;85:262-72.
[3]. Swenson AM, et al. Omecamtiv Mecarbil Enhances the Duty Ratio of Human β-Cardiac Myosin Resulting in Increased Calcium Sensitivity and Slowed Force Development in Cardiac Muscle. J Biol Chem. 2017 Mar 3;292(9):3768-3778.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C20H24FN5O3
Molecular Weight
401.43
CAS #
873697-71-3
SMILES
O=C(N1CCN(CC1)CC2=C(C(NC(NC3=CC=C(N=C3)C)=O)=CC=C2)F)OC
Synonyms
CK1827452; CK 1827452; CK1827452; Omecamtiv mecarbil.
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: 80 mg/mL (199.3 mM)
Water:<1 mg/mL
Ethanol: 6 mg/mL (14.9 mM)
Solubility (In Vivo)
1%DMSO+30% polyethylene glycol+1%Tween 80: 30 mg/mL
 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.4911 mL 12.4555 mL 24.9109 mL
5 mM 0.4982 mL 2.4911 mL 4.9822 mL
10 mM 0.2491 mL 1.2455 mL 2.4911 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

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Biological Data
  • Omecamtiv mecarbil

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