Mavacamten (MYK-461)

製品コードS8861 バッチS886103

印刷

化学情報

Chemical Structure Synonyms SAR439152 Storage
(From the date of receipt)		 3 years -20°C powder
化学式

C15H19N3O2
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
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <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.

溶剤液（一定の濃度）を調合する

生物活性

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.
in vitro

Mavacamten (MYK-461) primarily reduces the steady-state ATPase activity by inhibiting the rate of phosphate release of β-cardiac myosin-S1. It modulates multiple steps of the myosin chemomechanical cycle. In addition to decreasing the rate-limiting step of the cycle (phosphate release), this compound 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. It 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 this compound 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].

プロトコル(参考用のみ)

細胞アッセイ 細胞株 Mouse cardiac myofibrils
濃度 0.3 µM
反応時間 24 h
実験の流れ Mavacamten (MYK-461) was used to treat cells at various concentrations for 24 h.
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

参考

  • https://pubmed.ncbi.nlm.nih.gov/28808052/
  • https://pubmed.ncbi.nlm.nih.gov/26912705/

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

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
Evaluation of Neurotoxicity With Human Pluripotent Stem Cell-Derived Cerebral Organoids [ Curr Protoc, 2023, 3(4):e744] PubMed: 37068185
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。

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