Mavacamten (MYK-461)

Synonyms: SAR439152

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

Mavacamten (MYK-461) Chemical Structure

CAS: 1642288-47-8

Selleck's Mavacamten (MYK-461) has been cited by 3 publications

Purity & Quality Control

Batch: Purity: 99.92%
99.92

Mavacamten (MYK-461) Related Products

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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
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].

Cell Research Cell lines Mouse cardiac myofibrils
Concentrations 0.3 µM
Incubation Time 24 h
Method

Cells were treated with various concentrations of drug for 24 h.

In Vivo
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].

Animal Research 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
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06023186 Not yet recruiting
Obstructive Hypertrophic Cardiomyopathy
Michael Ayers|Bristol-Myers Squibb|University of Virginia
September 15 2023 --
NCT05489705 Recruiting
Obstructive Hypertrophic Cardiomyopathy
Bristol-Myers Squibb
August 16 2022 --
NCT04766892 Active not recruiting
Heart Failure With Preserved Ejection Fraction
Bristol-Myers Squibb
March 30 2021 Phase 2

Chemical Information & Solubility

Molecular Weight 273.33 Formula

C15H19N3O2

CAS No. 1642288-47-8 SDF --
Smiles CC(C)N1C(=O)C=C(NC1=O)NC(C)C2=CC=CC=C2
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 55 mg/mL ( (201.22 mM); Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 5 mg/mL

Water : Insoluble


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In vivo
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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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