1. Autophagy
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  3. Trimetazidine dihydrochloride

Trimetazidine dihydrochloride (Synonyms: 盐酸曲美他嗪)

目录号: HY-B0968 纯度: 99.62%
产品使用指南

Trimetazidine dihydrochloride 是一种选择性的长链 3-ketoyl coenzyme A thiolase 抑制剂,IC50 值为 75 nM,可抑制游离脂肪酸的 β-氧化。Trimetazidine dihydrochloride 是一种有效的抗心绞痛药和一种细胞保护药,具有抗氧化,抗炎,抗伤害和胃保护作用。Trimetazidine dihydrochloride 诱导自噬,还是一种 HADHA 抑制剂。

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Trimetazidine dihydrochloride Chemical Structure

Trimetazidine dihydrochloride Chemical Structure

CAS No. : 13171-25-0

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规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ¥550 In-stock
10 mg ¥500 In-stock
50 mg ¥800 In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

Other Forms of Trimetazidine dihydrochloride:

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Trimetazidine dihydrochloride is a selective long chain 3-ketoyl coenzyme A thiolase inhibitor with an IC50 of 75 nM, which can inhibit β-oxidation of free fatty acid (FFA). Trimetazidine dihydrochloride is an effective antianginal agent and a cytoprotective drug, has anti-oxidant, anti-inflammatory, antinociceptive and gastroprotective properties. Trimetazidine dihydrochloride triggers autophagy. Trimetazidine dihydrochloride is also a 3-hydroxyacyl-CoA dehydrogenase (HADHA) inhibitor[1][2][3][4].

IC50 & Target

IC50: 75 nM (long chain 3-ketoyl coenzyme A thiolase)[2]
β-oxidation[2]
Autophagy[3]
3-hydroxyacyl-CoA dehydrogenase (HADHA)[4]

体外研究
(In Vitro)

Trimetazidine (1 μM-100 μM; 24 hours; HUVECs) could enhance the viability of the injured HUVECs induces by oxidation in a certain dose-dependent manner[1].

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

Cell Viability Assay[1]

Cell Line: Human umbilical vein endothelial cells (HUVECs)
Concentration: 1 μM, 10 μM, 100 μM
Incubation Time: 24 hours
Result: Enhanced the viability of the injured HUVECs induced by oxidation.
体内研究
(In Vivo)

Trimetazidine (5-20 mg/kg; oral administration; 1 hour; Swiss albino male mice) in 10 mg/kg and 20 mg/kg doses significantly raises the seizure-threshold current in the increasing current electroshock seizure (ICES) test in the mice[5].

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

Animal Model: Swiss albino male mice (24-35 g)[4]
Dosage: 5 mg/kg, 10 mg/kg and 20 mg/kg;
10 mL/kg body weight
Administration: Oral administration; 1 hour
Result: In 10 mg/kg and 20 mg/kg doses significantly raised the seizure-threshold current in the ICES test.
Clinical Trial
分子量

339.26

Formula

C₁₄H₂₄Cl₂N₂O₃

CAS 号
中文名称

盐酸曲美他嗪

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

H2O : ≥ 100 mg/mL (294.76 mM)

DMSO : 25 mg/mL (73.69 mM; Need ultrasonic)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.9476 mL 14.7380 mL 29.4759 mL
5 mM 0.5895 mL 2.9476 mL 5.8952 mL
10 mM 0.2948 mL 1.4738 mL 2.9476 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: PBS

    Solubility: 100 mg/mL (294.76 mM); Clear solution; Need ultrasonic

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (7.37 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (7.37 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
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (7.37 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (7.37 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 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
*以上所有助溶剂都可在 MCE 网站选购。
参考文献
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
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The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2

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Trimetazidine dihydrochloride
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HY-B0968
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