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Mavacamten

CAS No. : 1642288-47-8

MCE 站：Mavacamten

产品活性：Mavacamten 是心肌肌球蛋白的调节剂，其在牛心脏和人心脏中的 IC₅₀ 值分别为 490，711 nM。

研究领域：Cytoskeleton

作用靶点：Myosin

In Vitro: Mavacamten is found to have an IC₅₀ value of 490 nM in the bovine system, 711 nM in the human system, and 2140 nM in the rabbit system, indicating selectivity of >4-fold for cardiac myosin.

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. 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.

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