(+)-EMD 57033
Based on 1 Customer Validation
(+)-EMD 57033 is a cardiac troponin C (cTnC) activator, is a dominant Ca2+ sensitizer. (+)-EMD 57033 binds the cardiac/slow skeletal troponin C isoform and exerts myocardial contractile promotion function.
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- Pureté: 98.69%
- CAS No.: 147527-31-9
- Formule: C22H23N3O4S
- Masse moléculaire:425.50
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Cardiac troponin C (cTnC)[1]
(+)-EMD 57033 (30 μM) recovers the activation and sensitivity of Ca2+ in pig single muscle fibres and reduces VIDD (ventilator-induced diaphragm muscle fibre dysfunction) of [2].
(+)-EMD 57033 (5.0-5.8 μM; 10-15 min) significantly increases the coronary blood flow and myocardial V o2 (O2 consumption) in both 100 bpm and 150 bpm heart rates of rabbit heart, with a [Ca2+]0 concentration-dependent manner ([Ca2+]0=1.0 or 2.5 mM)[3].
(+)-EMD 57033 (5.0-5.8 μM; 10-15 min) increases left ventricular (LV) end-diastolic pressure and prolongs relaxation[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mongrel dogs implanted with a micromanometer in left ventricle (LV) at the apex via lateral thoracotomy[4]
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Dosage:0.4 or 0.8 mg/kg/min
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Administration:Intravenous drip; infused over 20 minutes
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Result:Enhanced contractility at both doses, with similar changes in CON (conscious dogs) and HF (heart failure dogs) hearts.
Decreased the end-diastolic pressure (EDP) and lowered arterial load or preload at 0.8 mg/kg/min.
Chemical Information
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CAS No. 147527-31-9
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Appearance Solid
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Masse moléculaire 425.50
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Formule C22H23N3O4S
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Color White to off-white
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SMILES
O=C(N1CCCC2=C1C=CC(C3=NNC(SC3C)=O)=C2)C4=CC=C(OC)C(OC)=C4
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
DMSO : 100 mg/mL (235.02 mM; Need ultrasonic; 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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 (5.88 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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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.
Pureté et documentation
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Fiche technique (282 KB)
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SDS (558 KB)
- English - EN (558 KB)
- Français - FR (558 KB)
- Deutsch - DE (558 KB)
- Norwegian - NO (558 KB)
- Español - ES (558 KB)
- Swedish - SV (558 KB)
- Italian - IT (558 KB)
- Korean - KR (558 KB)
- Portuguese - PT (558 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Wang X, et al. Structure of the C-domain of human cardiac troponin C in complex with the Ca2+ sensitizing drug EMD 57033. J Biol Chem. 2001 Jul 6;276(27):25456-66. [Content Brief]
[2]. Ochala J, et al. EMD 57033 partially reverses ventilator-induced diaphragm muscle fibre calcium desensitisation. Pflugers Arch. 2010 Feb;459(3):475-83. [Content Brief]
[3]. Hgashiyama A, et al. Effects of EMD 57033 on contraction and relaxation in isolated rabbit hearts. Circulation. 1995 Nov 15;92(10):3094-104. [Content Brief]
[4]. Senzaki H, et al. Improved mechanoenergetics and cardiac rest and reserve function of in vivo failing heart by calcium sensitizer EMD-57033. Circulation. 2000 Mar 7;101(9):1040-8. [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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3502 mL | 11.7509 mL | 23.5018 mL | 58.7544 mL |
| 5 mM | 0.4700 mL | 2.3502 mL | 4.7004 mL | 11.7509 mL | |
| 10 mM | 0.2350 mL | 1.1751 mL | 2.3502 mL | 5.8754 mL | |
| 15 mM | 0.1567 mL | 0.7834 mL | 1.5668 mL | 3.9170 mL | |
| 20 mM | 0.1175 mL | 0.5875 mL | 1.1751 mL | 2.9377 mL | |
| 25 mM | 0.0940 mL | 0.4700 mL | 0.9401 mL | 2.3502 mL | |
| 30 mM | 0.0783 mL | 0.3917 mL | 0.7834 mL | 1.9585 mL | |
| 40 mM | 0.0588 mL | 0.2938 mL | 0.5875 mL | 1.4689 mL | |
| 50 mM | 0.0470 mL | 0.2350 mL | 0.4700 mL | 1.1751 mL | |
| 60 mM | 0.0392 mL | 0.1958 mL | 0.3917 mL | 0.9792 mL | |
| 80 mM | 0.0294 mL | 0.1469 mL | 0.2938 mL | 0.7344 mL | |
| 100 mM | 0.0235 mL | 0.1175 mL | 0.2350 mL | 0.5875 mL |
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