Sevasemten
Based on 1 Customer Validation
Sevasemten is an orally active, selective allosteric inhibitor of skeletal muscle myosin that protects skeletal muscle from contraction-induced injury. Sevasemten decreases muscle damage biomarkers and fibrosis while increasing muscle strength and activity in in Duchenne muscular dystrophy disease models.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.32%
- No. CAS: 2417395-15-2
- Fòrmula: C16H11F4N5O2
- Peso molecular:381.28
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Almacenamiento:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
Descripciòn
In Vitro
Sevasemten (0.01-10 μM, 1 h) inhibits fast myofibril ATPase from rabbit psoas muscle with an IC50 of 0.2 µM. EDG-5506 reduces the force of fast skeletal muscle fibers, protects mdx muscles from contraction damage, inhibits the intracellular calcium accumulation, as well as the destructive hypercontraction and clotting of fiber myoplasm[4].
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.
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Animal Model:Dog Duchenne muscular dystrophy models[4]
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Dosage:2 mg/kg
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Administration:2 mg/kg daily for 4 days, then every other day for the last 7 days
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Result:Reduced the creatine kinase activity in serum, increased the average daily activity, decreased the rest time.
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 2417395-15-2
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Appearance Solid
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Peso molecular 381.28
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Fòrmula C16H11F4N5O2
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Color White to off-white
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SMILES
O=C1C=CC(C2=CN=C(OCC(F)(F)F)N=C2)=NN1CC3=CC(F)=CN=C3
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Synonyms
EDG-5506
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
In Vitro:
DMSO : 250 mg/mL (655.69 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)
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: ≥ 2.08 mg/mL (5.46 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
In Vivo Dissolution Calculator
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.
Pureza y Documentación
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Ficha de datos (273 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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 | 2.6227 mL | 13.1137 mL | 26.2274 mL | 65.5686 mL |
| 5 mM | 0.5245 mL | 2.6227 mL | 5.2455 mL | 13.1137 mL | |
| 10 mM | 0.2623 mL | 1.3114 mL | 2.6227 mL | 6.5569 mL | |
| 15 mM | 0.1748 mL | 0.8742 mL | 1.7485 mL | 4.3712 mL | |
| 20 mM | 0.1311 mL | 0.6557 mL | 1.3114 mL | 3.2784 mL | |
| 25 mM | 0.1049 mL | 0.5245 mL | 1.0491 mL | 2.6227 mL | |
| 30 mM | 0.0874 mL | 0.4371 mL | 0.8742 mL | 2.1856 mL | |
| 40 mM | 0.0656 mL | 0.3278 mL | 0.6557 mL | 1.6392 mL | |
| 50 mM | 0.0525 mL | 0.2623 mL | 0.5245 mL | 1.3114 mL | |
| 60 mM | 0.0437 mL | 0.2186 mL | 0.4371 mL | 1.0928 mL | |
| 80 mM | 0.0328 mL | 0.1639 mL | 0.3278 mL | 0.8196 mL | |
| 100 mM | 0.0262 mL | 0.1311 mL | 0.2623 mL | 0.6557 mL |
Sevasemten Related Classifications
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