1. NF-κB Anti-infection Metabolic Enzyme/Protease Apoptosis
  2. NF-κB HIV Mitochondrial Metabolism Endogenous Metabolite Apoptosis
  3. α-Lipoic Acid

α-Lipoic Acid  (Synonyms: α-硫辛酸; Thioctic acid; (±)-α-Lipoic acid; DL-α-Lipoic acid)

目录号: HY-N0492 纯度: 99.86%
COA 产品使用指南

α-Lipoic Acid (Thioctic acid) 是一种抗氧化剂,是线粒体酶复合物的重要辅助因子。α-Lipoic Acid 可抑制 NF-κB 依赖性的 HIV-1 LTR 活化。α-Lipoic Acid 诱导内质网应激 (ERS) 介导的肝癌细胞凋亡 (apoptosis)。α-Lipoic Acid 可与 CPUL1 (HY-151802) 合成自组装的纳米聚合体 CPUL1-LA NA,其抗肿瘤效果优于 CPUL1

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α-Lipoic Acid Chemical Structure

α-Lipoic Acid Chemical Structure

CAS No. : 1077-28-7

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10 mM * 1 mL in DMSO ¥330
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500 mg ¥300
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1 g ¥420
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Other Forms of α-Lipoic Acid:

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  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

α-Lipoic Acid (Thioctic acid) is an antioxidant, which is an essential cofactor of mitochondrial enzyme complexes. α-Lipoic Acid inhibits NF-κB-dependent HIV-1 LTR activation[1][2][3]. α-Lipoic Acid induces endoplasmic reticulum (ER) stress-mediated apoptosis in hepatoma cells[4]. α-Lipoic Acid can be used with CPUL1 (HY-151802) to construct the self-assembled nanoaggregate CPUL1-LA NA, which has improved antitumor efficacy than CPUL1[5].

IC50 & Target[1][2]

Human Endogenous Metabolite

 

NF-κB

 

Mitochondrial bioenergetics

 

HIV-1

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 IC50
> 50 μM
Compound: alpha-thioctic acid
Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay
Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay
[PMID: 31202992]
Bel-7402 IC50
> 50 μM
Compound: alpha-thioctic acid
Antiproliferative activity against human Bel7402 cells assessed as reduction in cell viability after 72 hrs by MTT assay
Antiproliferative activity against human Bel7402 cells assessed as reduction in cell viability after 72 hrs by MTT assay
[PMID: 31202992]
K562 IC50
> 50 μM
Compound: alpha-thioctic acid
Antiproliferative activity against human K562 cells assessed as reduction in cell viability after 72 hrs by MTT assay
Antiproliferative activity against human K562 cells assessed as reduction in cell viability after 72 hrs by MTT assay
[PMID: 31202992]
L02 IC50
> 50 μM
Compound: alpha-thioctic acid
Cytotoxicity against human L02 cells assessed as reduction in cell viability after 72 hrs by MTT assay
Cytotoxicity against human L02 cells assessed as reduction in cell viability after 72 hrs by MTT assay
[PMID: 31202992]
PBMC IC50
> 50 μM
Compound: alpha-thioctic acid
Cytotoxicity against human PBMC assessed as reduction in cell viability after 72 hrs by MTT assay
Cytotoxicity against human PBMC assessed as reduction in cell viability after 72 hrs by MTT assay
[PMID: 31202992]
SGC-7901 IC50
> 50 μM
Compound: alpha-thioctic acid
Antiproliferative activity against human SGC7901 cells assessed as reduction in cell viability after 72 hrs by MTT assay
Antiproliferative activity against human SGC7901 cells assessed as reduction in cell viability after 72 hrs by MTT assay
[PMID: 31202992]
体外研究
(In Vitro)

The long terminal repeat (LTR) of HIV-1 is the target of cellular transcription factors such as NF-κB, and serves as the promoter-enhancer for the viral genome when integrated in host DNA[1]. α-Lipoic Acid (Alpha-Lipoic acid, ALA), a naturally occurring dithiol compound, plays an essential role in mitochondrial bioenergetics. α-Lipoic Acid reduces lipid accumulation in the liver by regulating the transcriptional factors SREBP-1, FoxO1, and Nrf2, and their downstream lipogenic targets via the activation of the SIRT1/LKB1/AMPK pathway. Treatment of cells with α-Lipoic Acid (250, 500 and 1000 μM) significantly increases the NAD+/NADH ratio in HepG2 cells (P<0.05 or P<0.01). Treatment with α-Lipoic Acid (50, 125, 250 and 500 μM) increases SIRT1 activity in HepG2 cells. α-Lipoic Acid (50, 125, 250, 500 and 1000 μM) increases phosphorylation of AMPK and acetyl-CoA carboxylase (ACC) in HepG2 cells in a dose-dependent fashion[1].

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

体内研究
(In Vivo)

C57BL/6J mice, divided into four groups, are fed an high-fat diet (HFD) for 24 weeks to induce nonalcoholic fatty liver disease (NAFLD) followed by daily administration of α-Lipoic Acid. Then, the effects of α-Lipoic Acid on hepatic lipid accumulation in long-term HFD-fed mice are assessed. Administration of α-Lipoic Acid (100 mg/kg or 200 mg/kg) markedly reduces visceral fat mass in mice. In addition, α-Lipoic Acid (100 mg/kg or 200 mg/kg) treatment inhibits the appetite and causes a dramatic weight loss (all P<0.05)[1].

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

Clinical Trial
分子量

206.33

Formula

C8H14O2S2

CAS 号
性状

固体

颜色

Light yellow to yellow

中文名称

α-硫辛酸

结构分类
初始来源
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 2 years
-20°C 1 year
溶解性数据
细胞实验: 

DMSO 中的溶解度 : 100 mg/mL (484.66 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

H2O 中的溶解度 : < 0.1 mg/mL (insoluble)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 4.8466 mL 24.2330 mL 48.4660 mL
5 mM 0.9693 mL 4.8466 mL 9.6932 mL
查看完整储备液配制表

* 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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物实验:

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

  • 方案 一

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

    Solubility: ≥ 2.5 mg/mL (12.12 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

    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;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

    生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
  • 方案 二

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

    Solubility: ≥ 2.5 mg/mL (12.12 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

    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。

    2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。

以下溶解方案,请直接配制工作液。建议现用现配,在短期内尽快用完。 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。

  • 方案 一

    请依序添加每种溶剂: 50% PEG300    50% Saline

    Solubility: 10 mg/mL (48.47 mM); 澄清溶液; 超声助溶

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
请输入您的动物体内配方组成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。
您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
连续给药周期超过半月以上,请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
纯度 & 产品资料

纯度: 99.86%

参考文献
Cell Assay
[1]

The human hepatocellular carcinoma (HepG2) cell line is cultured in Dulbecco's modified Eagle's medium containing 10% fetal bovine serum at 37°C and 5% CO2. HepG2 cells are treated with AMPK inhibitor (CC, 20 μM, 0.5 h), SIRT1 inhibitor (NA, 10 mM, 12 or 24 h), and AMPK activator (AICAR, 2 mM, 1 h), Palmitate (PA, 125 μM, 12 h) and α-Lipoic Acid (250 μM, 6 or 12 h)[1].

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

Animal Administration
[1]

Mice[1]
Male C57BL/6J mice (6-week-old; body weight: 22-24 g) are allowed ad libitum access to normal diet and water for 2 weeks before dividing into four groups (n=8): normal diet (ND) (10% energy from fat), high-fat diet (HFD) (60% energy from fat) and HFD plus α-Lipoic Acid (100 mg/kg or 200 mg/kg). After 24 weeks of treatment, blood samples are collected after the eyeballs of the mice are extracted for serum preparation by centrifugation at 2000×g for 10 min at 4°C. The liver tissues are harvested in liquid nitrogen and stored at -80°C.

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

参考文献

完整储备液配制表

* 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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 4.8466 mL 24.2330 mL 48.4660 mL 121.1651 mL
5 mM 0.9693 mL 4.8466 mL 9.6932 mL 24.2330 mL
10 mM 0.4847 mL 2.4233 mL 4.8466 mL 12.1165 mL
15 mM 0.3231 mL 1.6155 mL 3.2311 mL 8.0777 mL
20 mM 0.2423 mL 1.2117 mL 2.4233 mL 6.0583 mL
25 mM 0.1939 mL 0.9693 mL 1.9386 mL 4.8466 mL
30 mM 0.1616 mL 0.8078 mL 1.6155 mL 4.0388 mL
40 mM 0.1212 mL 0.6058 mL 1.2117 mL 3.0291 mL
50 mM 0.0969 mL 0.4847 mL 0.9693 mL 2.4233 mL
60 mM 0.0808 mL 0.4039 mL 0.8078 mL 2.0194 mL
80 mM 0.0606 mL 0.3029 mL 0.6058 mL 1.5146 mL
100 mM 0.0485 mL 0.2423 mL 0.4847 mL 1.2117 mL
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