Mavacamten (MYK-461)

Catalog No.S8861 Synonyms: SAR439152

For research use only.

Mavacamten (MYK-461, SAR439152) is a small-molecule modulator of cardiac myosin that targets the underlying sarcomere hypercontractility of hypertrophic cardiomyopathy (HCM), one of the most prevalent heritable cardiovascular disorders.

Mavacamten (MYK-461) Chemical Structure

CAS No. 1642288-47-8

Selleck's Mavacamten (MYK-461) has been cited by 2 Publications

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Biological Activity

Description Mavacamten (MYK-461, SAR439152) is a small-molecule modulator of cardiac myosin that targets the underlying sarcomere hypercontractility of hypertrophic cardiomyopathy (HCM), one of the most prevalent heritable cardiovascular disorders.
In vitro

MYK-461 primarily reduces the steady-state ATPase activity by inhibiting the rate of phosphate release of β-cardiac myosin-S1. MYK-461 modulates multiple steps of the myosin chemomechanical cycle. In addition to decreasing the rate-limiting step of the cycle (phosphate release), MYK-461 reduces the number of myosin-S1 heads that can interact with the actin thin filament during transition from the weakly to the strongly bound state without affecting the intrinsic rate. MYK-461 also decreases the rate of myosin binding to actin in the ADP-bound state and the ADP-release rate from myosin-S1 alone[1].

In vivo

Early, chronic administration of MYK-461 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[2].

Protocol (from reference)

Animal Research:

[2]

  • Animal Models: Young (ages 6 to 15 weeks) wild-type (WT) and HCM mice expressing α-cardiac myosin heavy chain missense mutations R403Q, R719W, or R453C
  • Dosages: 2.5 mg/kg
  • Administration: oral

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 273.33
Formula

C15H19N3O2

CAS No. 1642288-47-8
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC(C)N1C(=O)C=C(NC1=O)NC(C)C2=CC=CC=C2

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04766892 Recruiting Drug: mavacamten Heart Failure With Preserved Ejection Fraction Bristol-Myers Squibb March 30 2021 Phase 2
NCT04349072 Active not recruiting Drug: Mavacamten|Drug: Placebo HOCM Hypertrophic Obstructive Cardiomyopathy Bristol-Myers Squibb July 6 2020 Phase 3

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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