2. Cytoskeleton
  3. Myosin
  4. Sevasemten

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.

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Sevasemten Chemical Structure

Sevasemten Chemical Structure

CAS No. : 2417395-15-2

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Based on 1 publication(s) in Google Scholar

Sevasemten Related Antibodies

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Description

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[1][2][3][4].

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.

Sevasemten Related Antibodies
In Vivo

Sevasemten (2 mg/kg, po, once daily for 11 days) ameliorates the dog Duchenne muscular dystrophy, reduces the creatine kinase activity in serum, increases the average daily activity, and decreases the rest time in dog models[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Dog Duchenne muscular dystrophy models[4]
Dosage: 2 mg/kg
Administration: 2 mg/kg daily for 4 days, then every other day for the last 7 days
Result: Reduced the creatine kinase activity in serum, increased the average daily activity, decreased the rest time.
Molecular Weight

381.28

Formula

C16H11F4N5O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1C=CC(C2=CN=C(OCC(F)(F)F)N=C2)=NN1CC3=CC(F)=CN=C3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6227 mL 13.1137 mL 26.2274 mL
5 mM 0.5245 mL 2.6227 mL 5.2455 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

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C2

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V2

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.

  • Protocol 1

    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:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation
References

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
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Sevasemten Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Sevasemten2417395-15-2EDG-5506EDG5506EDG 5506Myosinorally activemyosinskeletal musclemuscle strength and activityInhibitorinhibitorinhibit

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