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Synonyms | SAR439152 | Storage (From the date of receipt) |
3 years -20°C powder | |
化学式 | C15H19N3O2 |
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分子量 | 273.33 | CAS No. | 1642288-47-8 | |
Solubility (25°C)* | 体外 | DMSO | 55 mg/mL (201.22 mM) | |
Ethanol | 14 mg/mL (51.22 mM) | |||
Water | Insoluble | |||
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
製品説明 | 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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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]. |
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]. |
細胞アッセイ | 細胞株 | Mouse cardiac myofibrils |
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濃度 | 0.3 µM | |
反応時間 | 24 h | |
実験の流れ | Cells were treated with various concentrations of drug for 24 h. |
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動物実験 | 動物モデル | Young (ages 6 to 15 weeks) wild-type (WT) and HCM mice expressing α-cardiac myosin heavy chain missense mutations R403Q, R719W, or R453C |
投薬量 | 2.5 mg/kg | |
投与方法 | oral |
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Right Ventricular Sarcomere Contractile Depression and the Role of Thick Filament Activation in Human Heart Failure With Pulmonary Hypertension [ Circulation, 2023, 147(25):1919-1932] | PubMed: 37194598 |
Right Ventricular Sarcomere Contractile Depression and the Role of Thick Filament Activation in Human Heart Failure With Pulmonary Hypertension [ Circulation, 2023, 147(25):1919-1932] | PubMed: 37194598 |
Mechanistic analysis of actin-binding compounds that affect the kinetics of cardiac myosin-actin interaction [ J Biol Chem, 2021, S0021-9258(21)00245-3] | PubMed: 33639160 |
Using hiPSC-CMs to Examine Mechanisms of Catecholaminergic Polymorphic Ventricular Tachycardia [ Curr Protoc, 2021, 1(12):e320] | PubMed: 34958715 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。