product name Omecamtiv mecarbil (CK-1827452)
Description: Omecamtiv mecarbil (also known as CK-1827452) is a specific 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.
References: Circ Heart Fail. 2010 Jul;3(4):522-7.
401.43
Formula
C20H24FN5O3
CAS No.
873697-71-3
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
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
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19399474
| In Vitro |
In vitro activity: In vitro, Omecamtiv mecarbil selectively activates cardiac myosin by increasing the myosin ATPase rate. 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. Kinase Assay: Cell Assay: |
|---|---|
| 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. 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. |
| Animal model | Sprague Dawley rats. |
| Formulation & Dosage | Dissolved in DMSO and then diluted in water; ≤1.2 mg/kg/hour; i.v. injection. |
| References | Circ Heart Fail. 2010 Jul;3(4):522-7. |
Related Posts
product name Omecamtiv mecarbil (CK-1827452)
Description: Omecamtiv mecarbil (also known as CK-1827452) is a specific 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.
References: Circ Heart Fail. 2010 Jul;3(4):522-7.
401.43
Formula
C20H24FN5O3
CAS No.
873697-71-3
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
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
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19399474
| In Vitro |
In vitro activity: In vitro, Omecamtiv mecarbil selectively activates cardiac myosin by increasing the myosin ATPase rate. 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. Kinase Assay: Cell Assay: |
|---|---|
| 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. 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. |
| Animal model | Sprague Dawley rats. |
| Formulation & Dosage | Dissolved in DMSO and then diluted in water; ≤1.2 mg/kg/hour; i.v. injection. |
| References | Circ Heart Fail. 2010 Jul;3(4):522-7. |