1. Cytoskeleton
  2. Myosin

Mavacamten (Synonyms: MYK461; SAR439152)

Cat. No.: HY-109037 Purity: >99.0%
Handling Instructions

Mavacamten is a modulator of cardiac myosin, with IC50s of 490, 711 nM for bovine cardiac and human cardiac, respectively.

For research use only. We do not sell to patients.

Mavacamten Chemical Structure

Mavacamten Chemical Structure

CAS No. : 1642288-47-8

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 571 In-stock
Estimated Time of Arrival: December 31
1 mg USD 190 In-stock
Estimated Time of Arrival: December 31
5 mg USD 390 In-stock
Estimated Time of Arrival: December 31
10 mg   Get quote  
50 mg   Get quote  

* Please select Quantity before adding items.

Featured Recommendations

Related Screening Libraries:

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Mavacamten is a 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].

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%. Treatment with Mavacamten eliminates SAM in 5/5 subjects, whereas SAM persists in 3/3 subjects treated with vehicle alone. Pressure gradients across the LVOT drop to 11.1±5.0 mmHg with Mavacamten treatment; whereas vehicle treated cats maintain stable LVOT pressure gradients[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].

Clinical Trial
Solvent & Solubility
In Vitro: 

10 mM in 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
10 mM 0.3659 mL 1.8293 mL 3.6586 mL
*Please refer to the solubility information to select the appropriate solvent.
References
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. Following imaging, the isoproterenol infusion is discontinued. When heart rate returns to baseline levels, a complete echocardiogram is performed on Mavacamten alone. Study drug is then discontinued, and animals are awakened, extubated and moved to recovery. Three of five cats are available to return for a control arm of this experiment after a 6-week washout period[2].

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

References
Molecular Weight

273.33

Formula

C₁₅H₁₉N₃O₂

CAS No.

1642288-47-8

SMILES

CC(N(C1=O)C(C=C(N[[email protected]](C2=CC=CC=C2)C)N1)=O)C

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Purity: >99.0%

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Inquiry Online

Your information is safe with us. * Required Fields.

Product name

 

Salutation

Applicant name *

 

Email address *

Phone number *

 

Organization name *

Country or Region *

 

Requested quantity *

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Mavacamten
Cat. No.:
HY-109037
Quantity:

Mavacamten

Cat. No.: HY-109037