| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| 1g |
|
||
| 5g |
|
||
| 10g |
|
||
| Other Sizes |
| Targets |
The targets include NF-κB (inhibition of NF-κB-dependent HIV-1 LTR activation), mitochondrial enzyme complexes (as an essential cofactor), and endoplasmic reticulum stress pathways (mediating apoptosis in hepatoma cells). It also functions as a general antioxidant.
|
|---|---|
| ln Vitro |
Cellular transcription factors like NF-κB target HIV-1's long terminal repeat (LTR), which when integrated into host DNA functions as a promoter-enhancer of the viral genome [1]. A naturally occurring dithiol molecule, alpha-lipoic acid (ALA) is essential to mitochondrial bioenergetics. Through controlling the transcription factors SREBP-1, FoxO1, and Nrf2 and their downstream lipogenic targets by triggering the SIRT1/LKB1/AMPK pathway, alpha-lipoic acid decreases fat buildup in the liver. HepG2 cells' NAD+/NADH ratio increased significantly (P<0.05 or P<0.01) when treated with α-lipoic acid at 250, 500, and 1000 μM. In HepG2 cells, treatment with α-lipoic acid at 50, 125, 250, and 500 μM enhanced SIRT1 activity. In HepG2 cells, alpha-lipoic acid (50, 125, 250, 500, and 1000 μM) stimulates AMPK and acetyl-CoA carboxylase (ACC) phosphorylation in a dose-dependent manner [1].
In vitro, α-Lipoic Acid sodium inhibits NF-κB-dependent HIV-1 LTR activation, induces endoplasmic reticulum stress-mediated apoptosis in hepatoma cells, and acts as an antioxidant. It can form self-assembled nano-polymers (CPUL1-LA NA) with enhanced antitumor efficacy. |
| ln Vivo |
To induce non-alcoholic fatty liver disease (NAFLD), four groups of C57BL/6J mice were given a high-fat diet (HFD) for 24 weeks. After that, the mice received daily doses of α-lipoic acid. Next, the impact of α-lipoic acid on the buildup of liver lipids in mice given a prolonged high-fat diet was assessed. When mice were given alpha-lipoic acid at doses of either 100 mg/kg or 200 mg/kg, their visceral fat mass was dramatically reduced. Furthermore, administration of α-lipoic acid at doses of 100 mg/kg or 200 mg/kg resulted in appetite suppression and a significant decrease in body weight (both P<0.05) [1].
In vivo, α-Lipoic Acid sodium is used as an antioxidant and metabolic modulator; it has been investigated for diabetic neuropathy, metabolic syndrome, and inflammatory conditions, and it can enhance the antitumor efficacy of co-administered agents in nano-polymer formulations. |
| Enzyme Assay |
NF-κB-dependent HIV-1 LTR activation is measured in reporter cells treated with α-Lipoic Acid sodium; luciferase activity is quantified, and NF-κB nuclear translocation is assessed by Western blotting. Antioxidant activity is measured by DPPH or ABTS radical-scavenging assays.
|
| Cell Assay |
Hepatoma cells or HIV-1 LTR reporter cells are treated with α-Lipoic Acid sodium; apoptosis is measured by caspase-3/7 activity or annexin V staining, ER stress markers (CHOP, GRP78) by Western blotting, and NF-κB activation by reporter assay.
|
| Animal Protocol |
Rats or mice with diabetic neuropathy or metabolic syndrome receive α-Lipoic Acid sodium by oral or intraperitoneal administration at doses selected from pharmacokinetic studies; nerve conduction velocity, oxidative stress markers, and metabolic parameters are measured, and tissue NF-κB activation is assessed.
|
| References |
|
| Molecular Formula |
C8H13NAO2S2
|
|---|---|
| Exact Mass |
228.025
|
| CAS # |
2319-84-8
|
| Related CAS # |
α-Lipoic Acid-d5; 1189471-66-6; α-Lipoic Acid; 1077-28-7; α-Lipoic Acid sodium; 2319-84-8
|
| PubChem CID |
23665026
|
| Appearance |
White to off-white solid powder
|
| Boiling Point |
362.5ºC at 760mmHg
|
| Melting Point |
241-253 °C
|
| Flash Point |
173ºC
|
| Vapour Pressure |
3.07E-06mmHg at 25°C
|
| Source |
Endogenously produced metabolite
|
| LogP |
1.45
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
5
|
| Heavy Atom Count |
13
|
| Complexity |
155
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
C(CCC(=O)[O-])CC1CCSS1.[Na+]
|
| InChi Key |
UUDFBRWLHZIIQX-UHFFFAOYSA-M
|
| InChi Code |
InChI=1S/C8H14O2S2.Na/c9-8(10)4-2-1-3-7-5-6-11-12-7;/h7H,1-6H2,(H,9,10);/q;+1/p-1
|
| Chemical Name |
sodium;5-(dithiolan-3-yl)pentanoate
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
H2O: ~35 mg/mL (~153.3 mM; with ultrasonication)
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
