Art. -Nr.: HY-109037

Mavacamten

(Synonyms: MYK461; SAR439152)

16 Cited Publications

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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.

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Reinheit: 99.94%
CAS. Nr.: 1642288-47-8
Formel: C₁₅H₁₉N₃O₂
Molecular Weight:273.34

Speicherung:

Powder -20°C, 3 years ; In solvent -80°C, 1 year , -20°C, 6 months

Mavacamten Chemical Structure

CAS. Nr.: 1642288-47-8

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (16)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Bioz

Biologische Aktivität

Beschreibung

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].

Alle Myosin Isoform-spezifische Produkte anzeigen :

MLCK

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.

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.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 1642288-47-8
Appearance Solid
Molecular Weight 273.34
Formel C₁₅H₁₉N₃O₂
Color White to off-white
SMILES

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

MYK461; SAR439152
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
In solvent	-80°C	1 year
	-20°C	6 months

Publications (16)

All 2D/3D Cell Culture and DifferentiationBio/Physico-chemical Assay

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Journal Impact Factor

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.
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.
JACC Basic Transl Sci

2025 Dec 19;11(1):101449.
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.
J Physiol

Myosin-binding protein C slows cardiac myofibril relaxation kinetics. [Abstract]

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.
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

Roles of cMyBP-C phosphorylation on cardiac contractile dysfunction in db/db mice. [Abstract]

2024 Jun:8:100075. PMID: 38957358
bioRxiv

2025 Jul 24.
bioRxiv

2025 Jun 30.
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

MYBPC3 D389V Variant Induces Hypercontractility in Cardiac Organoids. [Abstract]

2024 May 30:2024.05.29.596463. PMID: 38853909
bioRxiv

2024 Mar 27.
bioRxiv

2023 Apr 14.

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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.

Molaritätsrechner

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

Mass

Konzentration

Volumen

Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

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.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Protokoll

Animal Administration^[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) has not independently confirmed the accuracy of these methods. They are for reference only.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

Mavacamten

16 Cited Publications

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Mavacamten

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Publications Citing Use of MedChemExpress (MCE) Mavacamten

Alle Myosin Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (16)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Mavacamten

FDA-Approved Drug Library

Drug Repurposing Compound Library

Anti-Cardiovascular Disease Compound Library

Anti-COVID-19 Compound Library

Cytoskeleton Compound Library

Orally Active Compound Library

FDA Approved & Pharmacopeial Drug Library

Rare Diseases Drug Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Classic FDA-Approved Drug Library

3D Diverse Fragment Library

Publications Citing Use of MedChemExpress (MCE) Mavacamten

Alle Myosin Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (16)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Mavacamten Related Classifications

Art. -Nr.: HY-109037