2. Cytoskeleton
  3. Myosin
  4. Mavacamten

Mavacamten  (Synonyms: MYK461; SAR439152)

製品番号: HY-109037 純度: 99.94%
COA 取扱説明書 Technical Support

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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CAS 番号 : 1642288-47-8

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 99 在庫あり
Solution
10 mM * 1 mL in DMSO USD 99 在庫あり
Solid
1 mg $50 在庫あり
5 mg $90 在庫あり
10 mg $135 在庫あり
25 mg $230 在庫あり
50 mg $325 在庫あり
100 mg $455 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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カスタマーレビュー

Based on 16 publication(s) in Google Scholar

Other Forms of Mavacamten:

Mavacamten 関連抗体

Top Publications Citing Use of Products

    Mavacamten purchased from MedChemExpress. Usage Cited in: iScience. 2025 Oct 30;28(12):113901.  [Abstract]

    Nuclear stiffness of HCM-variants I79N and R92Q showed a significant decrease after 24-h 0.1 μM MAVA treatment. The HCM associated phenotype nuclei demonstrated values closer to their respective isogenic controls.

    Mavacamten purchased from MedChemExpress. Usage Cited in: Cell Rep Med. 2024 May 21;5(5):101520.  [Abstract]

    Beat amplitude: MYK-461 (75-300 nM) caused a dose-dependent decrease in beat amplitude in all HCM patient lines. Verapamil also reduced beat amplitude in all patient CMs, but this effect was lower than that seen with highest dose of MYK-461. Metoprolol had no effect.

    Mavacamten purchased from MedChemExpress. Usage Cited in: Cell Rep Med. 2024 May 21;5(5):101520.  [Abstract]

    ATPase activity: MYK-461 (300 nM; 30 min) decreased ATPase activity in 80, 81, and 82 CMs but not in 83 CMs. Verapamil and metoprolol had no effect.

    Mavacamten purchased from MedChemExpress. Usage Cited in: J Mol Cell Cardiol. 2024 Jun:191:27-39.  [Abstract]

    Representative OCR plot for both cell lines, with and without 1 hour treatment of 3 μM Mavacamten (Mava), including timepoint specific addition of electron transport chain modulating compounds.

    Mavacamten purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2024 Jan:170:116036.  [Abstract]

    Dose-response curves of Mavacamten and Verapamil. Lines presented as median (interquartile range) percentage of maximum contraction force. Grey dashed lines represent the half maximal inhibitory concentrations (IC50) of both drugs.

    Mavacamten purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2024 Jan:170:116036.  [Abstract]

    The effect of Mavacamten (1 μM) and Verapamil on the contractile curves of LMS, with Mavacamten prolonging the TTP. Exemplary tracings from a single LMS during each condition (before medication, after Verapamil, after Mavacamten). Verapamil and Mavacamten reduced twitch force (Ftwitch). Mavacamten increased time-to-peak (TTP) and time-to-relaxation (TTR), while Verapamil only increased TTR. Curves presented as compared to Ftwitch before drug administration. LMS = living myocardial slices.

    Myosin アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    MLCK

    • 生物活性

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    • 純度とドキュメンテーション

    • 参考文献

    • カスタマーレビュー

    製品説明

    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].
    体外実験

    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 関連抗体
    体内実験

    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.
    臨床実験
    分子量

    273.34

    分子式

    C15H19N3O2
    CAS 番号
    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
    輸送条件

    Room temperature in continental US; may vary elsewhere.
    保管条件
    Powder -20°C 3 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    DMSO : 83.33 mg/mL (304.86 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 3.6584 mL 18.2922 mL 36.5845 mL
    5 mM 0.7317 mL 3.6584 mL 7.3169 mL
    10 mM 0.3658 mL 1.8292 mL 3.6584 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.

    • Molarity Calculator

    • Dilution Calculator

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

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

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始）

    C1

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    体積 （開始）

    V1

    =
    濃度 （終了）

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    体内:

    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:

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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
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    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.
    純度とドキュメンテーション

    純度: 99.94%

    COA (248 KB) LCMS (93 KB)

    取扱説明書 (2659 KB)
    参考文献
    動物実験
    [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].

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    参考文献

    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 3.6584 mL 18.2922 mL 36.5845 mL 91.4612 mL
    5 mM 0.7317 mL 3.6584 mL 7.3169 mL 18.2922 mL
    10 mM 0.3658 mL 1.8292 mL 3.6584 mL 9.1461 mL
    15 mM 0.2439 mL 1.2195 mL 2.4390 mL 6.0974 mL
    20 mM 0.1829 mL 0.9146 mL 1.8292 mL 4.5731 mL
    25 mM 0.1463 mL 0.7317 mL 1.4634 mL 3.6584 mL
    30 mM 0.1219 mL 0.6097 mL 1.2195 mL 3.0487 mL
    40 mM 0.0915 mL 0.4573 mL 0.9146 mL 2.2865 mL
    50 mM 0.0732 mL 0.3658 mL 0.7317 mL 1.8292 mL
    60 mM 0.0610 mL 0.3049 mL 0.6097 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 0.3658 mL 0.9146 mL
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    Mavacamten Related Classifications

    • Molarity Calculator

    • Dilution Calculator

    The molarity calculator equation

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

    質量   濃度   体積   分子量 *
    = × ×

    The dilution calculator equation

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

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
    × = ×
    C1   V1   C2   V2
    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:

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

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