CK-1827452
1-Piperazinecarboxylic acid,4-[[2-fluoro-3-[[[(6-methyl-3-pyridinyl)amino]carbonyl]amino]phenyl]methyl]-, methyl ester
CAS: 873697-71-3
Molecular Formula: C20H24FN5O3
CK-1827452 - Names and Identifiers
CK-1827452 - Physico-chemical Properties
| Molecular Formula | C20H24FN5O3 |
| Molar Mass | 401.43 |
| Melting Point | 180℃ |
| Solubility | DMSO (Slightly), Methanol (Slightly) |
| Appearance | Solid |
| Color | White to Off-White |
| Storage Condition | -20°C Freezer |
| Use | Omecamtiv mecarbil (CK-1827452) is a specific myocardial myosin agonist and is a clinical drug for left ventricular systolic heart failure. |
| In vitro study | In vitro, Omecamtiv mecarbil selective activates cardiosin by increasing the myosin ATPase rate. In isolated cardiac myocytes, Omecamtiv mecarbil results in increased of myocyte contrast and alternatives of the myosin inhibitor BDM without increasing. In vitro, Omecamtiv mecarbil selectively activates cardiac myosin by increasing the myosin ATPase ratio. In isolated cardiomyocytes, Omecamtiv mcarbil leads to increased myocyte contractility and deactivates the myosin inhibitor BDM without increasing calcium transport or inhibiting the PDE pathway. |
| In vivo study | Omecamtiv mecarbil significantly increases fractional shortening starting at 0.4 mM plasma concentrations in SD rats, sham animals and in rats with heart failure. 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 emodynamic parameters. In SD rats, deep-water animals, and heart failure rats, Omecamtiv mcarbil significantly increased fractional shortening after a plasma concentration of 0.4 mM. In dogs with a conscious myocardial infarction (MI-sHF), Omecamtiv mcarbil significantly increased parietal ventricular thickness (25%), stroke volume (44%), cardiac output (22%) and left ventricle (LV) systolic ejection time (26%). In addition, Omecamtiv mecarbil also causes a decline in several hemodynamic parameters, including heart rate, mean left atrial pressure, and LV end diastolic pressure. In conscious dogs with left ventricular hypertrophy (LVH-sHF), omecentiv mcarbil had a similar and statistically differentiated effect on hemodynamic parameters. |
CK-1827452 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.491 ml | 12.455 ml | 24.911 ml |
| 5 mM | 0.498 ml | 2.491 ml | 4.982 ml |
| 10 mM | 0.249 ml | 1.246 ml | 2.491 ml |
| 5 mM | 0.05 ml | 0.249 ml | 0.498 ml |
Last Update：2024-01-02 23:10:35
CK-1827452 - Reference Information
| biological activity | Omecamtiv mcarbil (CK-1827452) is a specific cardiac myosin agonist, it is a clinical drug for left ventricular systolic heart failure. Phase 2. Omecamtiv mecarbil (CK-1827452) is a specific cardiac myosin agonist, which is a clinical drug for left ventricular systolic heart failure. Phase 2. |
| In vitro study | . In isolated cardiac myocytes, Omecamtiv mecarbil results in increased of myocyte contrast and alternatives of the myosin inhibitor BDM without increasing.|
| in vivo study | omecentiv mecarbil significant incremental shortening at 0.4 plasma concentrations in SD rats, sham animals and in rats with heart failure. In normal dogs with myocardial employment (MI-sHF), Omecamtiv mecarbil leads to a significant increase in wall thickness (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 emodynamic parameters. In SD rats, deep-water animals, and heart failure rats, Omecamtiv mcarbil significantly increased fractional shortening after a plasma concentration of 0.4 mM. In dogs with a conscious myocardial infarction (MI-sHF), Omecamtiv mcarbil significantly increased parietal ventricular thickness (25%), stroke volume (44%), cardiac output (22%) and left ventricle (LV) systolic ejection time (26%). In addition, Omecamtiv mecarbil also causes a decline in several hemodynamic parameters, including heart rate, mean left atrial pressure, and LV end diastolic pressure. In conscious dogs with left ventricular hypertrophy (LVH-sHF), omecentiv mcarbil had a similar and statistically differentiated effect on hemodynamic parameters. |
| Target | TargetValue Myosin ATPase |
| Target | Value |
Last Update：2024-04-10 22:29:15
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Product Name: Omecamtiv mecarbil Request for quotationCAS: 873697-71-3
Tel: 0712-8899838
Email: jy6101@rmastandards.com
Mobile: 86-15787876101
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Mobile: 18916960931
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Tel: +86-400-900-4166
Email: product@acmec-e.com
Mobile: +86-18621343501
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Tel: 609-228-6898
Email: sales@medchemexpress.com
tech@medchemexpress.com
Mobile: 609-228-6898
Spot supply
Product Name: Omecamtiv mecarbil Visit Supplier Webpage Request for quotationCAS: 873697-71-3
Tel: +16314854226
Email: info@bocsci.com
Mobile: +16314854226
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Product List: View Catalog
Spot supply
Product Name: Omecamtiv mecarbil (CK-1827452) Visit Supplier Webpage Request for quotationCAS: 873697-71-3
Tel: 18301782025
Email: 3008007409@qq.com
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