| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 250mg | |||
| Other Sizes |
| Targets |
α-Hydroxyglutaric acid targets several enzymes, acting as a competitive inhibitor of α-ketoglutarate-dependent dioxygenases. These include histone demethylases and DNA demethylases (TET enzymes), leading to epigenetic changes and altered gene expression. It is metabolized to 2-oxoglutarate by D- and L-2-hydroxyglutarate dehydrogenases.
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| ln Vitro |
Disodium alpha-hydroxyglutarate (2-hydroxyglutarate) inhibits the activity of several histone demethylases. α-hydroxyglutarate occupies the same space as α-KG in the active site of histone demethylases. Disodium α-hydroxyglutarate (2-hydroxyglutarate) inhibits the activity of TET 5-methylcytosine hydroxylase [1]. Treatment of U-87MG cells with disodium alpha-hydroxyglutarate (2-hydroxyglutarate; 10-50 mM) increases HIF-1α and decreases endostatin [1].
In vitro, α-hydroxyglutaric acid is used to study the effects of oncometabolites. It can inhibit α-ketoglutarate-dependent enzymes, leading to the accumulation of certain substrates and altered cellular metabolism. It is a key compound in cancer metabolism research, particularly for studying IDH-mutant tumors. |
| ln Vivo |
In vivo, the sodium salt of α-hydroxyglutaric acid is used in research to model the effects of IDH mutations. It can be administered to animals to study its impact on tumorigenesis or its role in metabolic disorders like 2-hydroxyglutaric aciduria. It is a research tool to understand the pathophysiology of these diseases.
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| Enzyme Assay |
In vitro enzyme assays for α-hydroxyglutaric acid measure its inhibition of α-ketoglutarate-dependent dioxygenases. The assay involves incubating the enzyme (e.g., a histone demethylase) with its substrate and α-ketoglutarate in the presence of the compound. The inhibition of the enzymatic reaction is measured, typically by detecting the product or by using a coupled assay.
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| Cell Assay |
In vitro cellular studies are conducted using cell lines, particularly those with IDH mutations. Cells are treated with the sodium salt of α-hydroxyglutaric acid, and its effects on histone methylation, DNA methylation, gene expression, and cell proliferation are studied. These studies help to elucidate the mechanisms of IDH-mutant cancers.
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| Animal Protocol |
In vivo animal experiments are performed by administering the compound to mice, often via injection. This can be used to elevate 2-HG levels in vivo to model the effects of IDH mutations. Endpoints include analysis of tumor development, epigenetic changes, and metabolic alterations in various tissues.
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| ADME/Pharmacokinetics |
α-Hydroxyglutaric Acid (sodium salt) has a molecular formula of C5H6Na2O5 and a molecular weight of 192.08 g/mol. It is a disodium salt. It is soluble in water and other polar solvents. For research, it is typically stored at -20°C, protected from moisture. Its purity is high for research-grade material.
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| Toxicity/Toxicokinetics |
As a research chemical, it is not intended for human therapeutic use. Its toxicological profile is related to its role as an oncometabolite. High levels of 2-HG can be toxic and are associated with disease. Standard laboratory safety precautions should be followed when handling it.
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| References | |
| Additional Infomation |
Disodium 2-hydroxyglutarate is an organic molecular entity.
α-Hydroxyglutaric Acid (sodium salt) is also known as 2-HG and is a well-known oncometabolite. It is a key compound in cancer metabolism research, particularly for studying IDH1/2-mutant tumors. It is also used in research on neurometabolic disorders and is available as a high-purity research standard. |
| Molecular Formula |
C5H6NA2O5
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|---|---|
| Molecular Weight |
192.0777
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| Exact Mass |
148.037
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| CAS # |
40951-21-1
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| Related CAS # |
2889-31-8 (Parent)
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| PubChem CID |
218623
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| Appearance |
White to off-white solid powder
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| Density |
1.5±0.1 g/cm3
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| Boiling Point |
394.2±27.0 °C at 760 mmHg
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| Melting Point |
>290ºC (dec.)
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| Flash Point |
206.4±20.2 °C
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| Vapour Pressure |
0.0±2.1 mmHg at 25°C
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| Index of Refraction |
1.520
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| LogP |
-1.45
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
12
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| Complexity |
130
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
DZHFTEDSQFPDPP-UHFFFAOYSA-L
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| InChi Code |
InChI=1S/C5H8O5.2Na/c6-3(5(9)10)1-2-4(7)8;;/h3,6H,1-2H2,(H,7,8)(H,9,10);;/q;2*+1/p-2
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| Chemical Name |
disodium;2-hydroxypentanedioate
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O : ~125 mg/mL (~650.77 mM)
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| 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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 5.2062 mL | 26.0308 mL | 52.0616 mL | |
| 5 mM | 1.0412 mL | 5.2062 mL | 10.4123 mL | |
| 10 mM | 0.5206 mL | 2.6031 mL | 5.2062 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
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.
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