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抑制剂/激活剂

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凋亡与自噬

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Mavacamten MYK461; SAR439152

Mavacamten (MYK461) 是具有口服活性的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。

货号：
TK0307
规格：

1mg

2mg

5mg
价格：
￥0.00

产品参数

CAS No.	1642288-47-8
生物活性	Mavacamten (MYK461) is an orally active modulator of cardiac myosin, with IC50s of 490, 711 nM for bovine cardiac and human cardiac, respectively.
分子式	C15H19N3O2
分子量	273.33
运输条件	Room temperature in continental US; may vary elsewhere.
储存条件	Powder -20°C 3 years
溶解性数据	DMSO : 83.33 mg/mL (304.87 mM; Need ultrasonic)
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.
体外研究	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.
纯度及产品资料	98%

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