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  3. Mavacamten

Mavacamten (Synonyms: MYK461; SAR439152)

目录号: HY-109037 纯度: 99.90%
产品使用指南

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。

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Mavacamten Chemical Structure

Mavacamten Chemical Structure

CAS No. : 1642288-47-8

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥1684
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1 mg ¥560
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5 mg ¥860
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10 mg ¥1320
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25 mg ¥2640
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50 mg ¥4400
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Top Publications Citing Use of Products
  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

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.

IC50 & Target

IC50: 490 nM (bovine cardiac), 711 nM (human cardiac)[1].

体外研究
(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[1].

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

体内研究
(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[2]. 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[3].

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

Clinical Trial
分子量

273.33

Formula

C15H19N3O2

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 83.33 mg/mL (304.87 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.6586 mL 18.2929 mL 36.5858 mL
5 mM 0.7317 mL 3.6586 mL 7.3172 mL
10 mM 0.3659 mL 1.8293 mL 3.6586 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (9.15 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (9.15 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液
  • 2.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (7.61 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (7.61 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 MCE 网站选购。
参考文献
Animal Administration
[2]

Cats[2]
Five cats are selected for study. At the completion of imaging, a tenminute intravenous infusion of Mavacamten (MYK-461 (n=5)) at 0.3 mg/kg/hr IV is started. Focused echocardiography is performed after five minutes. After ten minutes, the Mavacamten infusion rate is lowered to 0.12 mg/kg/hr IV, a blood sample is drawn and an echocardiogram performed. If ventricular function remains hypercontractile or within normal limits by visual inspection, another blood sample is obtained and the Mavacamten infusion rate is increased to 0.36 mg/kg/hr IV for ten minutes. Focused echocardiography is performed after five minutes. After ten minutes, the Mavacamten infusion rate is lowered to 0.15 mg/kg/hr IV, a blood sample is drawn and an echocardiogram performed[2].

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

参考文献

纯度: 99.90%

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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× = ×
C1   V1   C2   V2

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