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> Mavacamten [1642288-47-8]

Mavacamten [1642288-47-8]

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Mavacamten (MYK461) is an orally active modulator of cardiac myosin, with IC50s of 490, 711 nM for bovine cardiac and human cardiac, respectively.

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Mavacamten Estructura química

Mavacamten Estructura química

No. CAS : 1642288-47-8

This product is a controlled substance and not for sale in your territory.

Based on 8 publication(s) in Google Scholar

Other Forms of Mavacamten:

  • Mavacamten-d6 Obtener un presupuesto
  • Mavacamten-d1 Obtener un presupuesto
  • Mavacamten-d5 Obtener un presupuesto
Descripciòn

Mavacamten (MYK461) is an orally active modulator of cardiac myosin, with IC50s of 490, 711 nM for bovine cardiac and human cardiac, respectively.

IC50 & Target

IC50: 490 nM (bovine cardiac), 711 nM (human cardiac)[1].
In Vitro

Mavacamten is found to have an IC50 value of 490 nM in the bovine system, 711 nM in the human system, and 2140 nM in the rabbit system, indicating selectivity of >4-fold for cardiac myosin[1].

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

Mavacamten Related Antibodies
In Vivo

Treatment with Mavacamten reduces FS from 52±3% to 38±7%. Treatment with Mavacamten reduces FS from 81±7% to 60±13%, corresponding to a relative reduction of 25%. Across all measurements there is a linear correlation between FS and Mavacamten plasma concentrations with each 100 ng/mL increase in Mavacamten concentration lowering FS by 4.9%[2]. Mavacamten reduces contractility by decreasing the adenosine triphosphatase activity of the cardiac myosin heavy chain. Chronic administration of Mavacamten suppresses the development of ventricular hypertrophy, cardiomyocyte disarray, and myocardial fibrosis and attenuates hypertrophic and profibrotic gene expression in mice harboring heterozygous human mutations in the myosin heavy chain[3].

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

273.33

Fòrmula

C15H19N3O2
No. CAS

1642288-47-8
Appearance

Solid

Color

White to off-white

SMILES

CC(N(C1=O)C(C=C(N[C@H](C2=CC=CC=C2)C)N1)=O)C
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento
Powder -20°C 3 years
In solvent -80°C 1 year
-20°C 6 months
Solvente y solubilidad
In Vitro: 

DMSO : 83.33 mg/mL (304.87 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 3.6586 mL 18.2929 mL 36.5858 mL
5 mM 0.7317 mL 3.6586 mL 7.3172 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

  • Calculadora de molaridad

  • Calculadora de dilución

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

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: ≥ 2.5 mg/mL (9.15 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.08 mg/mL (7.61 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

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.
Pureza y Documentación

Purity: 99.94%

COA (248 KB) LCMS (93 KB)

Instrucciones de manejo (2659 KB)
Referencias

  • [1]. Kawas RF, et al. A small-molecule modulator of cardiac myosin acts on multiple stages of the myosin chemomechanical cycle. J Biol Chem. 2017 Oct 6;292(40):16571-16577.  [Content Brief]

    [2]. Stern JA, et al. A Small Molecule Inhibitor of Sarcomere Contractility Acutely Relieves Left Ventricular Outflow Tract Obstruction in Feline Hypertrophic Cardiomyopathy. PLoS One. 2016 Dec 14;11(12):e0168407.  [Content Brief]

    [3]. Green EM, et al. A small-molecule inhibitor of sarcomere contractility suppresses hypertrophic cardiomyopathy in mice. Science. 2016 Feb 5;351(6273):617-21.  [Content Brief]

Administraciòn de animales
[2]

Cats[2]
Five cats are selected for study. At the completion of imaging, a tenminute intravenous infusion of Mavacamten (MYK-461 (n=5)) at 0.3 mg/kg/hr IV is started. Focused echocardiography is performed after five minutes. After ten minutes, the Mavacamten infusion rate is lowered to 0.12 mg/kg/hr IV, a blood sample is drawn and an echocardiogram performed. If ventricular function remains hypercontractile or within normal limits by visual inspection, another blood sample is obtained and the Mavacamten infusion rate is increased to 0.36 mg/kg/hr IV for ten minutes. Focused echocardiography is performed after five minutes. After ten minutes, the Mavacamten infusion rate is lowered to 0.15 mg/kg/hr IV, a blood sample is drawn and an echocardiogram performed[2].

MCE no ha confirmado la precisión de estos métodos independientemente. Son solo para referencia.
Referencias

  • [1]. Kawas RF, et al. A small-molecule modulator of cardiac myosin acts on multiple stages of the myosin chemomechanical cycle. J Biol Chem. 2017 Oct 6;292(40):16571-16577.  [Content Brief]

    [2]. Stern JA, et al. A Small Molecule Inhibitor of Sarcomere Contractility Acutely Relieves Left Ventricular Outflow Tract Obstruction in Feline Hypertrophic Cardiomyopathy. PLoS One. 2016 Dec 14;11(12):e0168407.  [Content Brief]

    [3]. Green EM, et al. A small-molecule inhibitor of sarcomere contractility suppresses hypertrophic cardiomyopathy in mice. Science. 2016 Feb 5;351(6273):617-21.  [Content Brief]

  • [1]. Kawas RF, et al. A small-molecule modulator of cardiac myosin acts on multiple stages of the myosin chemomechanical cycle. J Biol Chem. 2017 Oct 6;292(40):16571-16577.

    [2]. Stern JA, et al. A Small Molecule Inhibitor of Sarcomere Contractility Acutely Relieves Left Ventricular Outflow Tract Obstruction in Feline Hypertrophic Cardiomyopathy. PLoS One. 2016 Dec 14;11(12):e0168407.

    [3]. Green EM, et al. A small-molecule inhibitor of sarcomere contractility suppresses hypertrophic cardiomyopathy in mice. Science. 2016 Feb 5;351(6273):617-21.

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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.6586 mL 18.2929 mL 36.5858 mL 91.4645 mL
5 mM 0.7317 mL 3.6586 mL 7.3172 mL 18.2929 mL
10 mM 0.3659 mL 1.8293 mL 3.6586 mL 9.1465 mL
15 mM 0.2439 mL 1.2195 mL 2.4391 mL 6.0976 mL
20 mM 0.1829 mL 0.9146 mL 1.8293 mL 4.5732 mL
25 mM 0.1463 mL 0.7317 mL 1.4634 mL 3.6586 mL
30 mM 0.1220 mL 0.6098 mL 1.2195 mL 3.0488 mL
40 mM 0.0915 mL 0.4573 mL 0.9146 mL 2.2866 mL
50 mM 0.0732 mL 0.3659 mL 0.7317 mL 1.8293 mL
60 mM 0.0610 mL 0.3049 mL 0.6098 mL 1.5244 mL
80 mM 0.0457 mL 0.2287 mL 0.4573 mL 1.1433 mL
100 mM 0.0366 mL 0.1829 mL 0.3659 mL 0.9146 mL
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Mavacamten Related Classifications

  • Cytoskeleton
  • Myosin
Help & FAQs

Keywords:

Mavacamten1642288-47-8MYK461 SAR439152MYK 461MYK-461SAR439152SAR 439152SAR-439152MyosinInhibitorinhibitorinhibit

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