Cat. No.: HY-N0492

α-Lipoic Acid

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

14 Cited Publications

Customer Review

Based on 14 publication(s) in Google Scholar

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. α-Lipoic Acid induces endoplasmic reticulum (ER) stress-mediated apoptosis in hepatoma cells. 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.

For research use only. We do not sell to patients.

Purity: 99.94%
CAS No.: 1077-28-7
Formula: C₈H₁₄O₂S₂
Molecular Weight:206.33

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

α-Lipoic Acid Chemical Structure

CAS No.: 1077-28-7

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (14)
Solvent & Solubility
- In Vitro
- In Vivo
Protocol
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

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

All NF-κB Isoforms :

All HIV Isoforms :

All Endogenous Metabolite Isoforms :

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]

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].

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

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].

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

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 1077-28-7
Appearance Solid
Molecular Weight 206.33
Formula C₈H₁₄O₂S₂
Color Light yellow to yellow
SMILES

O=C(O)CCCCC1SSCC1
Synonyms

Thioctic acid; (±)-α-Lipoic acid; DL-α-Lipoic acid
Structure Classification
- Ketones, Aldehydes, Acids
Initial Source
- Endogenous metabolite
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (14)

All WBIn Vivo Efficacy StudyCell Proliferation/Viability AssayIFIHC

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Journal Impact Factor

J Nanostructure Chem

13 May 2022.
Cell Biosci

FAK-dependent activation of src family kinase member BLK contributed to endometrial fibrosis via endoplasmic reticulum stress. [Abstract]

2025 Oct 31;15(1):150. PMID: 41174819

α-Lipoic Acid purchased from MedChemExpress. Usage Cited in: Cell Biosci. 2025 Oct 31;15(1):150. [Abstract]

Response experiments were performed in TGF-β1-induced hEndoSCs using siBlk and ERS activator (α-Lipoic Acid (α-LA)), successively. Detection of the protein expression levels by Western blot. In TGF-β1-induced hEndoSCs, Collagen I and α-SMA expression were downregulated by BLK knockdown using siBLK, and such inhibitory effect was counteracted by the ERS agonist α-Lipoic Acid (α-LA, 100 μM; 24 h).

α-Lipoic Acid purchased from MedChemExpress. Usage Cited in: Cell Biosci. 2025 Oct 31;15(1):150. [Abstract]

Immunofluorescence detected the effect of intervention ERS on the expression of Collagen I (red) and α-SMA (green), respectively. DAPI (blue) was used to stain nuclei. The results showed that the ERS agonist α-Lipoic Acid (α-LA, 100 μM; 24 h) further upregulated the expression of Collagen I and α-SMA induced by TGF-β1.
Inflammopharmacology

Therapeutic potential of alpha-lipoic acid on mitochondrial dynamics, oxidative/nitrosative stress, and histopathological changes in rat ulcerative colitis model. [Abstract]

2025 Sep;33(9):5563-5581. PMID: 40889013

α-Lipoic Acid purchased from MedChemExpress. Usage Cited in: Inflammopharmacology. 2025 Sep;33(9):5563-5581. [Abstract]

The macroscopic appearance and macroscopic scores of colon tissues were evaluated in all groups. Compared with the C group, the colon tissue damage characterized by ulceration, hyperemia and mucosal edema was significantly increased in the UC group, M group (50 mg/kg; oral gavage; once daily for 14 days; rats) and α-lipoic acid (ALA) group (100 mg/kg; oral gavage; once daily for 14 days; rats) (p < 0.01). The macroscopic score was lower in the M + ALA group than in other colitis-induced groups, although the difference was not statistically significant (*p* > 0.05).
Eur J Pharmacol

Alpha-lipoic acid alleviated intermittent hypoxia-induced myocardial injury in mice by promoting autophagy through Nrf2 signaling pathway. [Abstract]

2025 Feb 13:177380. PMID: 39954840
Int Immunopharmacol

α -Lipoic acid alleviates Parkinson's disease by suppressing S100A9-mediated pyroptosis. [Abstract]

2025 Apr 14:155:114539. PMID: 40233449

α-Lipoic Acid purchased from MedChemExpress. Usage Cited in: Int Immunopharmacol. 2025 Apr 14:155:114539. [Abstract]

SH-SY5Y cell viability reached 80% with α-Lipoic Acid (α-ALA) pretreatment at 150 μmol/L for 8 h.

α-Lipoic Acid purchased from MedChemExpress. Usage Cited in: Int Immunopharmacol. 2025 Apr 14:155:114539. [Abstract]

TH and α-Synuclein Expression Analysis: The expression of TH in the brains of the 6-OHDA group decreased, while both α-Lipoic Acid (α-ALA, 40 mg/kg; i.p.; once daily for 14 days) pretreatment and treatment significantly improved TH expression. In contrast, the expression of α-synuclein in the brains of the 6-OHDA group increased. α-ALA treatment alleviated this change, but α-ALA pretreatment did not show improvement.

α-Lipoic Acid purchased from MedChemExpress. Usage Cited in: Int Immunopharmacol. 2025 Apr 14:155:114539. [Abstract]

In the open field test, 6-OHDA reduced the movement distance, and both α-Lipoic Acid (α-ALA, 40 mg/kg; i.p.; once daily for 14 days; C57BL/6 mice) pretreatment and α-ALA treatment ameliorated this effect (n = 9–10).

α-Lipoic Acid purchased from MedChemExpress. Usage Cited in: Int Immunopharmacol. 2025 Apr 14:155:114539. [Abstract]

TH expression decreased in the 6-OHDA group, but increased in both the α-Lipoic Acid (α-ALA, 40 mg/kg; i.p.; once daily for 14 days; C57BL/6 mice) + 6-OHDA and 6-OHDA+α-ALA groups.

α-Lipoic Acid purchased from MedChemExpress. Usage Cited in: Int Immunopharmacol. 2025 Apr 14:155:114539. [Abstract]

α-Lipoic Acid (α-ALA, 40 mg/kg; i.p.; once daily for 14 days) pretreatment and treatment alleviated the upregulation of S100A9 protein expression induced by 6-OHDA in C57BL/6 mice, as validated by immunofluorescence analysis.
Biochim Biophys Acta Mol Basis Dis

Alpha-lipoic acid attenuates cardiac inflammation of CVB3 induced viral myocarditis via neutrophil-derived YM-1. [Abstract]

2025 Sep 7;1872(1):168034. PMID: 40925469
Virol Sin

α-Lipoic Acid Exerts Its Antiviral Effect against Viral Hemorrhagic Septicemia Virus (VHSV) by Promoting Upregulation of Antiviral Genes and Suppressing VHSV-Induced Oxidative Stress. [Abstract]

2021 Dec;36(6):1520-1531. PMID: 34510367
J Biochem Mol Toxicol

Isoquercitrin promotes ferroptosis and oxidative stress in nasopharyngeal carcinoma via the AMPK/NF-κB pathway. [Abstract]

2024 Jan;38(1):e23542. PMID: 37712196
Immun Inflamm Dis

Lipoic Acid Ameliorates Lipopolysaccharide-Induced Inflammation via Inhibition of Glycolysis in RAW264.7 Macrophages. [Abstract]

2026 Jan;14(1):e70313. PMID: 41503676
Vet Microbiol

The Chinese medicine monomer Schisandrin C inhibits PRRSV infection by regulating the OGT-PI3K/AKT/mTOR signaling pathway. [Abstract]

2026 May:316:110992. PMID: 41865607
Neurosci Lett

The mechanism of alpha-lipoic acid regulating dopaminergic neuronal damage in Parkinson's disease through the Nrf2/HMOX1 pathway. [Abstract]

2025 Aug 5:865:138338. PMID: 40763886
Res Sq

2025 Dec 4.
Oxid Med Cell Longev

α-Lipoic Acid Targeting PDK1/NRF2 Axis Contributes to the Apoptosis Effect of Lung Cancer Cells. [Abstract]

2021 Jun 4:2021:6633419. PMID: 34211631
Oncotarget

Synergistic neuroprotective effect of rasagiline and idebenone against retinal ischemia-reperfusion injury via the Lin28-let-7-Dicer pathway. [Abstract]

2018 Jan 30;9(15):12137-12153. PMID: 29552298

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (484.66 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : < 0.1 mg/mL (insoluble)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

4.8466 mL

24.2330 mL

48.4660 mL

5 mM

0.9693 mL

4.8466 mL

9.6932 mL

10 mM

0.4847 mL

2.4233 mL

4.8466 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (12.12 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (12.12 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (12.12 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 50% PEG300 50% Saline

Solubility: 10 mg/mL (48.47 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protocol

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].

MedChemExpress (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.

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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
SDS (597 KB)
- English - EN (597 KB)
- Français - FR (597 KB)
- Deutsch - DE (597 KB)
- Norwegian - NO (597 KB)
- Español - ES (597 KB)
- Swedish - SV (597 KB)
- Italian - IT (597 KB)
- Korean - KR (597 KB)
- Portuguese - PT (597 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Xiao L, et al. Activity of the dietary antioxidant ergothioneine in a virus gene-based assay for inhibitors of HIV transcription. Biofactors. 2006;27(1-4):157-65. [Content Brief]

[2]. Lei D, et al. Synergistic neuroprotective effect of rasagiline and idebenone against retinal ischemia-reperfusion injury via the Lin28-let-7-Dicer pathway. Oncotarget. 2018 Jan 30;9(15):12137-12153. [Content Brief]

[3]. Yang Y, et al. Alpha-lipoic acid improves high-fat diet-induced hepatic steatosis by modulating the transcription factors SREBP-1, FoxO1 and Nrf2 via the SIRT1/LKB1/AMPK pathway. J Nutr Biochem. 2014 Nov;25(11):1207-1217. [Content Brief]

[4]. Pibiri M, et al. α-Lipoic acid induces Endoplasmic Reticulum stress-mediated apoptosis in hepatoma cells. Sci Rep. 2020 Apr 28;10(1):7139. [Content Brief]

[5]. Liu J, et al. Nanoaggregates of Disulfide-Decorated TrxR Inhibitor Promote Cellular Uptake, Selective Targeting, and Antitumor Efficacy. Langmuir, 2022.

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	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

α-Lipoic Acid

14 Cited Publications

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α-Lipoic Acid

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Publications Citing Use of MedChemExpress (MCE) α-Lipoic Acid

All NF-κB Isoforms

All HIV Isoforms

All Endogenous Metabolite Isoforms

Biological Activity

Chemical Information

Publications (14)

Solvent & Solubility

Protocol