Information Mavacamten (MYK-461) 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. 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.
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Mavacamten (MYK-461)
CAS number：1642288-47-8 molecular formula：C15H19N3O2
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| Chinese alias | - | ||
| English alias | EX-A2072 | MYK-461; Mavacamten; SAR439152 | Camzyos | HY-109037 | PLLA(10k)-mPEG(1k) | GTPL11265 | 6-(((1S)-1-phenylethyl)amino)-3-(propan-2-yl)pyrimidine-2,4(1H,3H)-dione | Mavacamten [INN] | QX45B99R3J | 6-{[(1S)-1-phenylethyl]amino}-3-(propan-2-yl)-1,2 | ||
| CAS number | 1642288-47-8 | molecular formula | C15H19N3O2 |
| molecular weight | 273.33 g/mol | Exact mass | - |
| PSA | 61.400 Ų | logp | 2.093 |
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