Omecamtiv mecarbil (CK-1827452)

Catalog No.S2623 Batch:S262304

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Technical Data

Formula

C20H24FN5O3

Molecular Weight 401.43 CAS No. 873697-71-3
Solubility (25°C)* In vitro DMSO 80 mg/mL (199.28 mM)
Ethanol 80 mg/mL (199.28 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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 Study:[1]
  • Animal Models

    Sprague Dawley rats.

  • Dosages

    ≤1.2 mg/kg/hour

  • Administration

    Administered via i.v.

Customer Product Validation

Data from [Data independently produced by University of Illinois at Chicago, 2014]

Data from [Data independently produced by , , J Physiol, 2018, 596(1):31-46]

Selleck's Omecamtiv mecarbil (CK-1827452) has been cited by 33 publications

Characterization of NEB pathogenic variants in patients reveals novel nemaline myopathy disease mechanisms and omecamtiv mecarbil force effects [ Acta Neuropathol, 2024, 147(1):72] PubMed: 38634969
Deconvolution of polygenic risk score in single cells unravels cellular and molecular heterogeneity of complex human diseases [ bioRxiv, 2024, 2024.05.14.594252] PubMed: 38798507
Clinically Relevant Models of Cardiac Function using Human Stem Cell-derived Cardiomyocytes [ , 2023, ] PubMed: none
The force of the myosin motor sets cooperativity in thin filament activation of skeletal muscles [ Commun Biol, 2022, 5(1):1266] PubMed: 36400920
Effects of omecamtiv mecarbil and mavacamten in isolated human atrium [ Naunyn Schmiedebergs Arch Pharmacol, 2022, 10.1007/s00210-022-02333-0] PubMed: 36399186
Myosin with hypertrophic cardiac mutation R712L has a decreased working stroke which is rescued by omecamtiv mecarbil [ Elife, 2021, 10e63691] PubMed: 33605878
Mechanistic analysis of actin-binding compounds that affect the kinetics of cardiac myosin-actin interaction [ J Biol Chem, 2021, S0021-9258(21)00245-3] PubMed: 33639160
Generative adversarial networks for construction of virtual populations of mechanistic models: simulations to study Omecamtiv Mecarbil action [ J Pharmacokinet Pharmacodyn, 2021, 10.1007/s10928-021-09787-4] PubMed: 34716531
Development and Application of NovelIn VitroAssays to Advance Drug Discovery for Arrhythmogenic Cardiomyopathy and Respiratory Syncytial Virus Infection [ ProQuest , 2021, 28718834] PubMed: none
Orthophosphate increases the efficiency of slow muscle-myosin isoform in the presence of omecamtiv mecarbil [ Nat Commun, 2020, 11(1):3405] PubMed: 32636378

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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