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S88459

MYK-461 (SAR-439152)

源叶(MedMol) 98%
  • 英文名:
  • MYK-461 (SAR-439152)
  • 别名:
  • CAS号:
  • 1642288-47-8
  • 分子式:
  • C15H19N3O2
  • 分子量:
  •  273.33
  • 核磁/质谱:
品牌货号产品规格价格(RMB) 库存(上海) 北京 武汉 南京 数量计量单位 加入购物车...
源叶(MedMol) S88459-1mg 98% ¥320.00元 >10 - - - EA 加入购物车
源叶(MedMol) S88459-5mg 98% ¥570.00元 >10 - - - EA 加入购物车
源叶(MedMol) S88459-10mg 98% ¥950.00元 >10 - - - EA 加入购物车
源叶(MedMol) S88459-25mg 98% ¥1890.00元 >10 - - - EA 加入购物车
源叶(MedMol) S88459-50mg 98% ¥2900.00元 >10 - - - EA 加入购物车
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  • 产品描述:

    Mavacamten (MYK461) is an orally active modulator of cardiac myosin, with IC50s of 490, 711 nM for bovine cardiac and human cardiac, respectively.

  • 靶点: IC50: 490 nM (bovine cardiac), 711 nM (human cardiac);Myosin
  • 体内研究:
    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. 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
  • 参考文献:
    1. Kawas RF, et al. A small-molecule modulator of cardiac myosin acts on multiple stages of the myosin chemomechanical cycle. J Biol Chem. 2017 Oct 6;292(40):16571-16577. 2. Stern JA, et al. A Small Molecule Inhibitor of Sarcomere Contractility Acutely Relieves Left Ventricular Outflow Tract Obstruction in Feline Hypertrophic Cardiomyopathy. PLoS One. 2016 Dec 14;11(12):e0168407. 3. Green EM, et al. A small-molecule inhibitor of sarcomere contractility suppresses hypertrophic cardiomyopathy in mice. Science. 2016 Feb 5;351(6273):617-21.
  • 溶解性: Soluble  in  DMSO
  • 保存条件: -20℃
  • 配置溶液浓度参考:
    1mg 5mg 10mg
    1 mM 0 ml 0 ml 0 ml
    5 mM 0 ml 0 ml 0 ml
    10 mM 0 ml 0 ml 0 ml
    50 mM 0 ml 0 ml 0 ml
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