| Size | Price | Stock | Qty |
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| 50mg |
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| Other Sizes |
| Targets |
DL-threo-3-Hydroxyaspartic acid targets excitatory amino acid transporters (EAATs), specifically human EAAT1 and EAAT2. It inhibits glutamate uptake in COS-1 cells expressing human EAAT1 with an IC₅₀ of 96 μM and EAAT2 with an IC₅₀ of 31 μM. By blocking glutamate transporters, the compound increases extracellular glutamate levels, which can be used to study glutamatergic neurotransmission and excitotoxicity. Its inhibitory activity makes it a valuable tool for neuroscience research.
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| ln Vitro |
In vitro, DL-threo-3-Hydroxyaspartic acid inhibits glutamate uptake in COS-1 cells expressing human EAAT1 (IC₅₀ = 96 μM) and EAAT2 (IC₅₀ = 31 μM). It acts as a glutamate uptake inhibitor by blocking excitatory amino acid transporters. The compound's activity has been characterized in cell-based assays measuring glutamate transport. Its inhibitory potency is higher against EAAT2 than EAAT1, suggesting some selectivity between transporter subtypes.
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| ln Vivo |
In vivo, DL-threo-3-Hydroxyaspartic acid blocks glutamate transport in cannulated Sprague-Dawley rats. By inhibiting glutamate uptake, the compound increases extracellular glutamate levels, which can be used to study the role of glutamate transporters in synaptic function and excitotoxicity. The compound has been used as a tool to investigate glutamate transport mechanisms in vivo. However, detailed in vivo efficacy data are not extensively published.
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| Enzyme Assay |
In vitro transporter inhibition assays for DL-threo-3-Hydroxyaspartic acid involve measuring glutamate uptake in cells expressing EAATs. COS-1 cells or other cell lines expressing human EAAT1 or EAAT2 are incubated with radiolabeled glutamate ([³H]glutamate) in the presence of varying concentrations of the inhibitor. Uptake is measured by scintillation counting, and IC₅₀ values are calculated from dose-response curves. The compound's purity is confirmed by HPLC.
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| Cell Assay |
In vitro cellular assays for DL-threo-3-Hydroxyaspartic acid typically involve evaluation of glutamate uptake in cell lines expressing EAATs. COS-1 cells or other suitable cell lines are transfected with human EAAT1 or EAAT2 and used for uptake assays. Cells are treated with the compound and [³H]glutamate, and uptake is measured. Cytotoxicity may be assessed using standard cell viability assays. The compound is stored as powder at -20°C for 3 years or 4°C for 2 years.
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| Animal Protocol |
In vivo animal experiments for DL-threo-3-Hydroxyaspartic acid typically involve cannulated Sprague-Dawley rats. The compound is administered via intracerebral or systemic routes, and glutamate transport inhibition is evaluated by measuring extracellular glutamate levels using microdialysis. Behavioral or electrophysiological endpoints may also be assessed to study the functional consequences of glutamate transporter inhibition.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of DL-threo-3-Hydroxyaspartic acid are characteristic of small amino acid derivatives. The compound has a molecular weight of 149.10 g/mol and molecular formula C₄H₇NO₅. As a polar amino acid analog, it is expected to have limited oral bioavailability but may be administered via injection for central nervous system studies. The compound is stored as powder at -20°C for 3 years or 4°C for 2 years; in solvent at -80°C for 6 months or -20°C for 1 month.
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| Toxicity/Toxicokinetics |
The toxicological profile of DL-threo-3-Hydroxyaspartic acid is not extensively documented. As a glutamate uptake inhibitor, it may have neurotoxic potential at high concentrations due to increased extracellular glutamate and excitotoxicity. Comprehensive toxicological evaluations including acute toxicity and repeated-dose studies have not been reported. Standard laboratory safety precautions should be followed when handling this compound.
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| References | |
| Additional Infomation |
(3S)-3-hydroxy-L-aspartic acid is the (3S)-diastereomer of 3-hydroxy-L-aspartic acid and is a metabolite. It is the conjugate acid of (3S)-3-hydroxy-L-aspartic acid (2-) and (3S)-3-hydroxy-L-aspartic acid (1-), and also the enantiomer of (3R)-3-hydroxy-D-aspartic acid. (3S)-3-hydroxy-L-aspartic acid is a metabolite found or produced in Saccharomyces cerevisiae.
DL-threo-3-Hydroxyaspartic acid (CAS# 4294-45-5, molecular formula C₄H₇NO₅, molecular weight 149.10) is a glutamate uptake inhibitor that blocks glutamate transport. It inhibits EAAT1 (IC₅₀ = 96 μM) and EAAT2 (IC₅₀ = 31 μM). No clinical trials or regulatory approvals have been identified. Storage: powder at -20°C for 3 years or 4°C for 2 years. |
| Molecular Formula |
C4H7NO5
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|---|---|
| Molecular Weight |
149.10208
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| Exact Mass |
149.032
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| CAS # |
4294-45-5
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| Related CAS # |
L-threo-3-Hydroxyaspartic acid;7298-99-9
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| PubChem CID |
443239
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| Appearance |
White to off-white solid powder
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| Density |
1.738 g/cm3
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| Boiling Point |
368.7ºC at 760 mmHg
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| Melting Point |
>230ºC dec
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| Flash Point |
176.8ºC
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| Index of Refraction |
1.583
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| LogP |
-4.4
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
10
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| Complexity |
156
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| Defined Atom Stereocenter Count |
2
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| SMILES |
OC(C(C(C(=O)O)O)N)=O
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| InChi Key |
YYLQUHNPNCGKJQ-LWMBPPNESA-N
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| InChi Code |
InChI=1S/C4H7NO5/c5-1(3(7)8)2(6)4(9)10/h1-2,6H,5H2,(H,7,8)(H,9,10)/t1-,2-/m0/s1
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| Chemical Name |
(2S,3S)-2-amino-3-hydroxybutanedioic acid
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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 |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 6.7069 mL | 33.5345 mL | 67.0691 mL | |
| 5 mM | 1.3414 mL | 6.7069 mL | 13.4138 mL | |
| 10 mM | 0.6707 mL | 3.3535 mL | 6.7069 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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