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Mavacamten (MYK-461)

Name: Mavacamten (MYK-461)
Brand: Selleck Chemicals
SKU: S8861
Rating: 5 (3 reviews)

Synonyms: SAR439152

Catalog No.S8861 Purity:99.92%

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

Purity & Quality Control

Batch: Purity: 99.92%

99.92

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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
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT06338202	Not yet recruiting	Obstructive Hypertrophic Cardiomyopathy (oHCM)	Bristol-Myers Squibb	April 1 2024	--
NCT06253221	Recruiting	Cardiomyopathy Hypertrophic	Bristol-Myers Squibb	April 17 2024	Phase 3
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

References

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	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years -20°C powder		1 month-20°Cin solvent

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
Batch:

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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.

Handling Instructions

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