Mavacamten（MYK-461）

Cas No.:	1642288-47-8
Chemical Name:	Mavacamten
Synonyms:	Mavacamten;QX45B99R3J;(S)-3-isopropyl-6-((1-phenylethyl)amino)pyrimidine-2,4(1H,3H)-dione;Mavacamten [INN];Mavacamten [WHO-DD];MYK461;GTPL11265;s8861;SAR439152;DB14921;SB19779;(S)-3-Isopropyl-6-((1-phenylethyl)amino) pyrimidine-2,4(1H,3H)-dione;(S)-3-Isopropyl-6-((1-phenylethyl)amino)pyrimidine-2, 4(1H,3H)-dione;(S)-3-Isopropyl-6
SMILES:	O=C1N([H])C(=C([H])C(N1C([H])(C([H])([H])[H])C([H])([H])[H])=O)N([H])[C@@]([H])(C([H])([H])[H])C1C([H])=C([H])C([H])=C([H])C=1[H]
Formula:	C15N3O2H19
M.Wt:	273.3303
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:	Mavacamten is a modulator of cardiac myosin, with IC50s of 490, 711 nM for bovine cardiac and human cardiac, respectively.
In Vivo:	Treatment with Mavacamten reduces FS from 52±3% to 38±7%. Treatment with Mavacamten reduces FS from 81±7% to 60±13%, corresponding to a relative reduction of 25%. Across all measurements there is a linear correlation between FS and Mavacamten plasma concentrations with each 100 ng/mL increase in Mavacamten concentration lowering FS by 4.9%. Treatment with Mavacamten eliminates SAM in 5/5 subjects, whereas SAM persists in 3/3 subjects treated with vehicle alone. Pressure gradients across the LVOT drop to 11.1±5.0 mmHg with Mavacamten treatment; whereas vehicle treated cats maintain stable LVOT pressure gradients[2]. Mavacamten reduces contractility by decreasing the adenosine triphosphatase activity of the cardiac myosin heavy chain. Chronic administration of Mavacamten 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[3].
In Vitro:	Mavacamten is a modulator of cardiac myosin, with IC50s of 490, 711 nM for bovine cardiac and human cardiac, respectively.