Mavacamten-d₆  (Synonyms: MYK461-d₆; SAR439152-d₆)

Mavacamten-d₆ (MYK461-d₆; SAR439152-d₆) is deuterium labeled Mavacamten (HY-109037). Mavacamten (MYK461) is an orally active modulator of cardiac myosin, with IC₅₀s of 490, 711 nM for bovine cardiac and human cardiac, respectively.

氢、碳和其他元素的稳定重同位素已被纳入药物分子中，主要作为药物开发过程中定量的示踪剂。氘化引起了人们的关注，因为它可能影响药物的药代动力学和代谢谱^[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

279.37

C₁₅H₁₃D₆N₃O₂

2453251-18-6

1642288-47-8

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-216.  [Content Brief]

  [2]. 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.  [Content Brief]

  [3]. 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.  [Content Brief]

  [4]. Green EM, et al. A small-molecule inhibitor of sarcomere contractility suppresses hypertrophic cardiomyopathy in mice. Science. 2016 Feb 5;351(6273):617-21.  [Content Brief]