For research use only.
Catalog No.S8861 Synonyms: SAR439152
CAS No. 1642288-47-8
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.
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|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.|
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.
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.
|In vitro||DMSO||55 mg/mL (201.22 mM)|
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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||MyoKardia Inc.||March 30 2021||Phase 2|
|NCT04349072||Recruiting||Drug: Mavacamten|Drug: Placebo||HOCM Hypertrophic Obstructive Cardiomyopathy||MyoKardia Inc.||June 26 2020||Phase 3|
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