Omecamtiv mecarbil
Based on 4 publication(s) in Google Scholar
Omecamtiv mecarbil (CK-1827452) is a selective cardiac myosin activator.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.83%
- No. CAS: 873697-71-3
- Fòrmula: C20H24FN5O3
- Peso molecular:401.43
-
Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Actividad biológica
-
Chemical Information
-
Solvente y solubilidad
- Pureza y Documentación
- Referencias
-
Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Omecamtiv mecarbil
More
Customer Validation & Images
-
Bio/Physico-chemical Assay
-
Bio/Physico-chemical Assay
-
Bio/Physico-chemical Assay
-
Bio/Physico-chemical Assay
-
Bio/Physico-chemical Assay
Actividad biológica
Descripciòn
In Vitro
Omecamtiv mecarbil (10 μM) reduces the maximal ATPase (kcat) 4.5-fold and dramatically reduces the actin concentration at which ATPase is half-maximal (KATPase) 30-fold. The Omecamtiv mecarbil-induced inhibition of the actin-activated ATPase is evaluated in a concentration-dependent manner to determine the EC50 (0.52 ± 0.10 μM). Omecamtiv mecarbil does not change the overall actin affinity. Omecamtiv mecarbil traps a population of myosin heads in a weak actin affinity state with slow product release. Omecamtiv mecarbil can reduce the actin sliding velocity more than 100-fold in the in vitro motility assay[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
-
No. CAS 873697-71-3
-
Appearance Solid
-
Peso molecular 401.43
-
Fòrmula C20H24FN5O3
-
Color White to off-white
-
SMILES
O=C(N1CCN(CC1)CC2=C(C(NC(NC3=CC=C(N=C3)C)=O)=CC=C2)F)OC
-
Synonyms
CK-1827452
-
Envío
Room temperature in continental US; may vary elsewhere.
-
Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (4)
-
Journal Impact Factor
-
Most Recent
-
Biomedicines
Characterization of Stimulatory Action on Voltage-Gated Na+ Currents Caused by Omecamtiv Mecarbil, Known to Be a Myosin Activator. [Abstract]2023 May 3;11(5):1351. PMID: 37239022
Omecamtiv mecarbil purchased from MedChemExpress. Usage Cited in: Biomedicines. 2023 May 3;11(5):1351. [Abstract]
Representative current traces achieved in the control period, with the presence of Omecamtiv mecarbil (OM) (3-10 µM), and washout of Omecamtiv mecarbil (OM).
Omecamtiv mecarbil purchased from MedChemExpress. Usage Cited in: Biomedicines. 2023 May 3;11(5):1351. [Abstract]
Concentration-dependent relationship of Omecamtiv mecarbil (OM) (0.3-100 µM) on the transient (INa(T), red open circles) and late (INa(L), black filled squares) components of INa evoked by short membrane depolarization.
Omecamtiv mecarbil purchased from MedChemExpress. Usage Cited in: Biomedicines. 2023 May 3;11(5):1351. [Abstract]
Quasi steady state inactivation curve of INa(T) taken with (red open circles) or without the addition (black filled circles) of Omecamtiv mecarbil (OM) (10 µM).
Omecamtiv mecarbil purchased from MedChemExpress. Usage Cited in: Biomedicines. 2023 May 3;11(5):1351. [Abstract]
The relationship of the relative INa(T) versus the PT duration obtained without (black filled circles) or with (red open circles) the application of Omecamtiv mecarbil (OM) (10 µM).
Omecamtiv mecarbil purchased from MedChemExpress. Usage Cited in: Biomedicines. 2023 May 3;11(5):1351. [Abstract]
The relationship of the relative amplitude of INa versus the stimulus duration achieved without (black filled circles) and with (red open circles) the presence of Omecamtiv mecarbil (OM) (10 µM).
-
J Gen Physiol
Fluorescence lifetime-based assay reports structural changes in cardiac muscle mediated by effectors of contractile regulation. [Abstract]2023 Mar 6;155(3):e202113054. PMID: 36633587 -
J Mol Cell Cardiol Plus
Omecamtiv mecarbil in precision-cut living heart failure slices: A story of a double-edged sword. [Abstract]2023 Jul 22:5:100040. PMID: 39802172 -
Cureus
Lack of Effect of Omecamtiv Mecarbil on Smooth Muscle Myosin Phosphatase Target Subunit-1 (MYPT1) Phosphorylation and Hemodynamics in Rats. [Abstract]2025 Jul 13;17(7):e87854. PMID: 40799893
Solvente y solubilidad
In Vitro:
DMSO : 20 mg/mL (49.82 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.23 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.23 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
-
Ficha de datos (272 KB)
-
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
-
Instrucciones de manejo (2659 KB)
Referencias
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4911 mL | 12.4555 mL | 24.9109 mL | 62.2774 mL |
| 5 mM | 0.4982 mL | 2.4911 mL | 4.9822 mL | 12.4555 mL | |
| 10 mM | 0.2491 mL | 1.2455 mL | 2.4911 mL | 6.2277 mL | |
| 15 mM | 0.1661 mL | 0.8304 mL | 1.6607 mL | 4.1518 mL | |
| 20 mM | 0.1246 mL | 0.6228 mL | 1.2455 mL | 3.1139 mL | |
| 25 mM | 0.0996 mL | 0.4982 mL | 0.9964 mL | 2.4911 mL | |
| 30 mM | 0.0830 mL | 0.4152 mL | 0.8304 mL | 2.0759 mL | |
| 40 mM | 0.0623 mL | 0.3114 mL | 0.6228 mL | 1.5569 mL |
Omecamtiv mecarbil Related Classifications
HY-14233 Related Classifications
Powered by Bioz