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  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)

目錄號: HY-N0492 純度: 99.86%
COA 產(chǎn)品使用指南

α-Lipoic Acid (Thioctic acid) 是一種抗氧化劑,是線粒體酶復合物的重要輔助因子。α-Lipoic Acid 可抑制 NF-κB 依賴性的 HIV-1 LTR 活化。α-Lipoic Acid 誘導內(nèi)質(zhì)網(wǎng)應激 (ERS) 介導的肝癌細胞凋亡 (apoptosis)。α-Lipoic Acid 可與 CPUL1 (HY-151802) 合成自組裝的納米聚合體 CPUL1-LA NA,其抗腫瘤效果優(yōu)于 CPUL1

MCE 的所有產(chǎn)品僅用作科學研究或藥證申報,我們不為任何個人用途提供產(chǎn)品和服務

α-Lipoic Acid Chemical Structure

α-Lipoic Acid Chemical Structure

CAS No. : 1077-28-7

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規(guī)格 價格 是否有貨 數(shù)量
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

  • 實驗參考方法

  • 純度 & 產(chǎn)品資料

  • 參考文獻

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

 

細胞效力
(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]
體外研究
(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.

體內(nèi)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 號
性狀

固體

顏色

Light yellow to yellow

中文名稱

α-硫辛酸

結(jié)構(gòu)分類
初始來源
運輸條件

Room temperature in continental US; may vary elsewhere.

儲存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性數(shù)據(jù)
細胞實驗: 

DMSO 中的溶解度 : 100 mg/mL (484.66 mM; 超聲助溶; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響,請使用新開封的 DMSO)

H2O 中的溶解度 : < 0.1 mg/mL (insoluble)

配制儲備液
濃度 溶劑體積 質(zhì)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
查看完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C儲存時,請在2年內(nèi)使用, -20°C儲存時,請在1年內(nèi)使用。

  • 摩爾計算器

  • 稀釋計算器

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

質(zhì)量
=
濃度
×
體積
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動物實驗:

請根據(jù)您的 實驗動物和給藥方式 選擇適當?shù)娜芙夥桨浮?

以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液,再依次添加助溶劑:
——為保證實驗結(jié)果的可靠性,澄清的儲備液可以根據(jù)儲存條件,適當保存;體內(nèi)實驗的工作液,建議您現(xiàn)用現(xiàn)配,當天使用;
以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比;如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過加熱和/或超聲的方式助溶

  • 方案 一

    請依序添加每種溶劑: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

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

    此方案可獲得 ≥ 2.5 mg/mL(飽和度未知)的澄清溶液。

    1 mL 工作液為例,取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 400 μL PEG300 中,混合均勻;再向上述體系中加入 50 μL Tween-80,混合均勻;然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL

    生理鹽水的配制:將 0.9 g 氯化鈉,溶解于 ddH?O 并定容至 100 mL,可以得到澄清透明的生理鹽水溶液。
  • 方案 二

    請依序添加每種溶劑: 10% DMSO    90% (20% SBE-β-CD in Saline)

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

    此方案可獲得 ≥ 2.5 mg/mL(飽和度未知)的澄清溶液。

    1 mL 工作液為例,取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液 中,混合均勻。

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

以下溶解方案,請直接配制工作液。建議現(xiàn)用現(xiàn)配,在短期內(nèi)盡快用完。 以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比; 如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過加熱和/或超聲的方式助溶。

  • 方案 一

    請依序添加每種溶劑: 50% PEG300    50% Saline

    Solubility: 10 mg/mL (48.47 mM); 澄清溶液; 超聲助溶

動物溶解方案計算器
請輸入動物實驗的基本信息:

給藥劑量

mg/kg

動物的平均體重

g

每只動物的給藥體積

μL

動物數(shù)量

由于實驗過程有損耗,建議您多配一只動物的量
請輸入您的動物體內(nèi)配方組成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的動物是免疫缺陷鼠或者體弱鼠,建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。
方案所需 助溶劑 包括:DMSO, ,均可在 MCE 網(wǎng)站選購。 Tween 80,均可在 MCE 網(wǎng)站選購。
計算結(jié)果
工作液所需濃度 : mg/mL
儲備液配制方法 : mg 藥物溶于 μL  DMSO(母液濃度為 mg/mL)。
您所需的儲備液濃度超過該產(chǎn)品的實測溶解度,以下方案僅供參考,如有需要,請與 MCE 中國技術支持聯(lián)系。
動物實驗體內(nèi)工作液的配制方法 : 取 μL DMSO 儲備液,加入 μL 。 μL ,混合均勻至澄清,再加 μL Tween 80,混合均勻至澄清,再加 μL 生理鹽水。
連續(xù)給藥周期超過半月以上,請謹慎選擇該方案。
請確保第一步儲備液溶解至澄清狀態(tài),從左到右依次添加助溶劑。您可采用超聲加熱 (超聲清洗儀,建議頻次 20-40 kHz),渦旋吹打等方式輔助溶解。
純度 & 產(chǎn)品資料

純度: 99.86%

參考文獻
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.

參考文獻

完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C儲存時,請在2年內(nèi)使用, -20°C儲存時,請在1年內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)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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產(chǎn)品名稱:
α-Lipoic Acid
目錄號:
HY-N0492
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