Omecamtiv mecarbil (Synonyms: CK-1827452; CK1827452) |
| Katalog-Nr.GC12832 |
Omecamtiv mecarbil (CK-1827452) ist ein selektiver kardialer Myosinaktivator.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 873697-71-3
Sample solution is provided at 25 µL, 10mM.
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Omecamtiv mecarbil (CK-1827452) is the first potent cardiac myosin activator that can specifically activate the cardiac myosin S1 domain but not other muscle myosins. In clinical trials, omecamtiv mecarbil has been considered as a promising therapeutic approach to treat systolic heart failure1.
Omecamtiv mecarbil accelerates the actin-dependent Pi release from cardiac myosin S1 domain, thus increases the rate of transition from weakly actin-bound state to strongly actin-bound state (EC50= 2.3 μM)1.
At the concentration of 200nM, omecamtiv mecarbil was reported to remarkably increase the contractility of adult rat cardiac myocytes without influencing calcium transient. In vivo, Omecamtiv mecarbil has been shown to improve cardiac function without changing myocardial oxygen consumption in both beagle dogs and Sprague-Dawley rats under isoflurane anesthesia1.
References:
1. Malik FI1, Hartman JJ, Elias KA, Morgan BP, Rodriguez H, Brejc K, Anderson RL, Sueoka SH, Lee KH, Finer JT, Sakowicz R, Baliga R, Cox DR, Garard M,Godinez G, Kawas R, Kraynack E, Lenzi D, Lu PP, Muci A, Niu C, Qian X, Pierce DW, Pokrovskii M, Suehiro I, Sylvester S, Tochimoto T, Valdez C, Wang W,Katori T, Kass DA, Shen YT, Vatner SF, Morgans DJ. Cardiac myosin activation: a potential therapeutic approach for systolic heart failure. Science. 2011 Mar 18;331(6023):1439-43.
| Cell experiment [1]: | |
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Cell lines |
Cardiac myocytes |
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Preparation method |
The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20 °C for several months. |
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Reaction Conditions |
200 nM |
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Applications |
Omecamtiv Mecarbil extended the duration of contraction without affecting the rates of contraction or relaxation. In addition, Omecamtiv Mecarbil also increased myocyte contraction in the presence of a β-adrenergic blocker, Carvedilol. |
| Animal experiment [1]: | |
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Animal models |
Conscious and heart failure dogs |
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Dosage form |
A bolus at 0.5 mg/kg, followed by infusion at 0.5 mg/kg per hr |
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Applications |
In a conscious canine model, Omecamtiv Mecarbil improved left ventricular systolic function. In heart failure dogs, Omecamtiv Mecarbil significantly increased stroke volume and cardiac output. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1]. Malik FI1, Hartman JJ, Elias KA, Morgan BP, Rodriguez H, Brejc K, Anderson RL, Sueoka SH, Lee KH, Finer JT, Sakowicz R, Baliga R, Cox DR, Garard M,Godinez G, Kawas R, Kraynack E, Lenzi D, Lu PP, Muci A, Niu C, Qian X, Pierce DW, Pokrovskii M, Suehiro I, Sylvester S, Tochimoto T, Valdez C, Wang W,Katori T, Kass DA, Shen YT, Vatner SF, Morgans DJ. Cardiac myosin activation: a potential therapeutic approach for systolic heart failure. Science. 2011 Mar 18;331(6023):1439-43. |
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| Cas No. | 873697-71-3 | SDF | |
| Überlieferungen | CK-1827452; CK1827452 | ||
| Chemical Name | methyl 4-[[2-fluoro-3-[(6-methylpyridin-3-yl)carbamoylamino]phenyl]methyl]piperazine-1-carboxylate | ||
| Canonical SMILES | CC1=NC=C(C=C1)NC(=O)NC2=CC=CC(=C2F)CN3CCN(CC3)C(=O)OC | ||
| Formula | C20H24FN5O3 | M.Wt | 401.43 |
| Löslichkeit | ≥ 19.1mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 16 reference(s) in Google Scholar.)
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