货号	规格	价格	上海	北京	珠海	重庆	武汉
S88459-1mg买3赠1	99.10%	￥260.00 S88459-1mg ￥260.00 现货（买3赠1）	4574 >10	-	-	-	-
S88459-5mg买3赠1	99.10%	￥450.00 S88459-5mg ￥450.00 现货（买3赠1）	918 >10	-	-	-	-
S88459-10mg买3赠1	99.10%	￥720.00 S88459-10mg ￥720.00 现货（买3赠1）	458 >10	-	-	-	-
S88459-25mg买3赠1	99.10%	￥1440.00 S88459-25mg ￥1440.00 现货（买3赠1）	185 >10	-	-	-	-
S88459-50mg买3赠1	99.10%	￥2210.00 S88459-50mg ￥2210.00 现货（买3赠1）	94 >10	-	-	-	-

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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

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

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分子摩尔量

计算重置

MYK-461 (SAR-439152)