Mavacamten
Based on 16 publication(s) in Google Scholar
Mavacamten (MYK461) is an orally active modulator of cardiac myosin, with IC50s of 490, 711 nM for bovine cardiac and human cardiac, respectively.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.94%
- CAS 番号: 1642288-47-8
- 分子式: C15H19N3O2
- 分子量:273.34
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保管条件:Powder -20°C, 3 years ; In solvent -80°C, 1 year , -20°C, 6 months
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生物活性
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化学情報
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溶剤 & 溶解度
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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MedChemExpress（MCE）の使用を引用している文献 Mavacamten
More- Nat Commun. 2026 Feb 14. [Abstract]
- Cell Rep Med. 2024 May 21;5(5):101520. [Abstract]
- Biomed Pharmacother. 2024 Jan:170:116036. [Abstract]
- JACC Basic Transl Sci. 2025 Dec 19;11(1):101449.
- J Mol Cell Cardiol. 2024 Jun:191:27-39. [Abstract]
- J Physiol. 2025 Oct;603(19):5351-5368. [Abstract]
- iScience. 2025 Oct 30;28(12):113901. [Abstract]
- Cardiovasc Drugs Ther. 2025 Jan 4. [Abstract]
- J Gen Physiol. 2023 Mar 6;155(3):e202113054. [Abstract]
- J Mol Cell Cardiol Plus. 2024 Jun:8:100075. [Abstract]
- bioRxiv. 2025 Jul 24.
- bioRxiv. 2025 Jun 30.
- bioRxiv. 2025 May 18:2025.05.14.654110. [Abstract]
- bioRxiv. 2024 May 30:2024.05.29.596463. [Abstract]
- bioRxiv. 2024 Mar 27.
- bioRxiv. 2023 Apr 14.
Customer Validation & Images
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2D/3D Cell Culture and Differentiation
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2D/3D Cell Culture and Differentiation
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Bio/Physico-chemical Assay
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2D/3D Cell Culture and Differentiation
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Bio/Physico-chemical Assay
生物活性
IC50: 490 nM (bovine cardiac), 711 nM (human cardiac)[1].
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 1642288-47-8
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性状 Solid
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分子量 273.34
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分子式 C15H19N3O2
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Color White to off-white
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SMILES
CC(N(C1=O)C(C=C(N[C@H](C2=CC=CC=C2)C)N1)=O)C
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別名
MYK461; SAR439152
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years In solvent -80°C 1 year -20°C 6 months
Publications (16)
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Journal Impact Factor
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Most Recent
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Nat Commun
GLP-1 activates KATP channels in coronary pericytes as the effector of brain-gut-heart signalling mediating cardioprotection. [Abstract]2026 Feb 14. PMID: 41690912 -
Cell Rep Med
Myosin inhibitor reverses hypertrophic cardiomyopathy in genotypically diverse pediatric iPSC-cardiomyocytes to mirror variant correction. [Abstract]2024 May 21;5(5):101520. PMID: 38642550
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.
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Biomed Pharmacother
Biomechanical response of ultrathin slices of hypertrophic cardiomyopathy tissue to myosin modulator mavacamten. [Abstract]2024 Jan:170:116036. PMID: 38134635
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.
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J Mol Cell Cardiol
MYBPC3-c.772G>A mutation results in haploinsufficiency and altered myosin cycling kinetics in a patient induced stem cell derived cardiomyocyte model of hypertrophic cardiomyopathy. [Abstract]2024 Jun:191:27-39. PMID: 38648963
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.
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J Physiol
2025 Oct;603(19):5351-5368. PMID: 40936293 -
iScience
Phenotype specific nuclear lamina remodeling in hiPSC derived cardiomyocytes bearing TNNT2 sarcomeric variants. [Abstract]2025 Oct 30;28(12):113901. PMID: 41321620
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.
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Cardiovasc Drugs Ther
Novel Selective Cardiac Myosin-Targeted Inhibitors Alleviate Myocardial Ischaemia-Reperfusion Injury. [Abstract]2025 Jan 4. PMID: 39754660 -
J Gen Physiol
Fluorescence lifetime-based assay reports structural changes in cardiac muscle mediated by effectors of contractile regulation. [Abstract]2023 Mar 6;155(3):e202113054. PMID: 36633587 -
J Mol Cell Cardiol Plus
2024 Jun:8:100075. PMID: 38957358 -
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bioRxiv
Myosin modulator Aficamten inhibits force in cardiac muscle by altering myosin's biochemical activity without changing thick filament structure. [Abstract]2025 May 18:2025.05.14.654110. PMID: 40463178 -
bioRxiv
2024 May 30:2024.05.29.596463. PMID: 38853909 -
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溶剤 & 溶解度
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)
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.
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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 (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.
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.
プロトコル
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) has not independently confirmed the accuracy of these methods. They are for reference only.
純度とドキュメンテーション
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データシート (276 KB)
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取扱説明書 (2659 KB)
参考文献
[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]
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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