DL-TBOA
Based on 1 publication(s) in Google Scholar
DL-TBOA is a potent non-transportable inhibitor of excitatory amino acid transporters with IC50s of 70 μM, 6 μM and 6 μM for excitatory amino acid transporter-1 (EAAT1), EAAT2 and EAAT3, respectively. DL-TBOA inhibits the uptake of [14C]glutamate in COS-1 cells expressing the human EAAT1 and EAAT2 with Ki valuesof 42 μM and 5.7 μM, respectively. DL-TBOA blocks EAAT4 and EAAT5 in a competitive manner with Ki values of 4.4 μM and 3.2 μM, respectively.
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- Pureté: 99.54%
- CAS No.: 205309-81-5
- Formule: C11H13NO5
- Masse moléculaire:239.23
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) DL-TBOA
More
Activité biologique
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EAAT1 |
EAAT2 |
EAAT3 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| COS-1 | IC50 |
7 μM
Compound: L-TBOA
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Inhibition of [14C]glutamate uptake at human EAAT3 expressed in african green monkey COS1 cells
Inhibition of [14C]glutamate uptake at human EAAT3 expressed in african green monkey COS1 cells
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[PMID: 18650095] |
| HEK293 | IC50 |
0.96 μM
Compound: TBOA
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Inhibition of [3H]-D-Asp uptake at human EAAT2 expressed in HEK293 cells measured after 3 mins by TopCount method
Inhibition of [3H]-D-Asp uptake at human EAAT2 expressed in HEK293 cells measured after 3 mins by TopCount method
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[PMID: 27636002] |
| HEK293 | IC50 |
1.6 μM
Compound: TBOA
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Inhibition of [3H]-D-Asp uptake at human EAAT1 expressed in HEK293 cells measured after 3 mins by TopCount method
Inhibition of [3H]-D-Asp uptake at human EAAT1 expressed in HEK293 cells measured after 3 mins by TopCount method
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[PMID: 27636002] |
| HEK293 | IC50 |
3.7 μM
Compound: TBOA
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Inhibition of [3H]-D-Asp uptake at human EAAT3 expressed in HEK293 cells measured after 3 mins by TopCount method
Inhibition of [3H]-D-Asp uptake at human EAAT3 expressed in HEK293 cells measured after 3 mins by TopCount method
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[PMID: 27636002] |
| MDCK | IC50 |
1.3 μM
Compound: L-TBOA
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Glutamate uptake inhibition assay on glutamate transporters (excitatory amino acid transporters EAAT2) stably expressed on MDCK cells before U.V radiation
Glutamate uptake inhibition assay on glutamate transporters (excitatory amino acid transporters EAAT2) stably expressed on MDCK cells before U.V radiation
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[PMID: 12617931] |
DL-TBOA (70-350 μM; 48 hours; HCT116 and LoVo cell lines) treatment concentration-dependently enhances SN38-induced loss of viability. DL-TBOA reversed Oxaliplatin-induced loss of viability[4].
DL-TBOA (350 μM; 24 hours; HCT116 and LoVo cell lines) treatment decreases p53 induction by SN38 and oxaliplatin[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCT116 and LoVo cell lines
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Concentration:70 μM, 350 μM
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Incubation Time:48 hours
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Result:Enhanced SN38-induced, and counteracted Oxaliplatin-induced, cell death.
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Cell Line:HCT116 and LoVo cell lines
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Concentration:350 μM
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Incubation Time:24 hours
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Result:p53 induction by SN38 and oxaliplatin was decreased.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Sprague-Dawley rats (180-250 g)[5]
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Dosage:1 nmol, 3 nmol, 10 nmol
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Administration:Intracerebroventricularly injection (i.c.v.)
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Result:Dose dependently facilitated various somatic signs induced by Naloxone (0.1 mg/kg).
Chemical Information
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CAS No. 205309-81-5
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Appearance Solid
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Masse moléculaire 239.23
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Formule C11H13NO5
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Color White to off-white
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SMILES
OC([C@@H](N)[C@@H](C(O)=O)OCC1=CC=CC=C1)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
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Cell Chem Biol
Electrochemical sensor toolkit for simultaneous glutamate detection at edge of cleft and peri-soma. [Abstract]2025 Jun 19;32(6):885-898.e11. PMID: 40466640
Solvant et solubilité
DMSO : 200 mg/mL (836.02 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 5 mg/mL (20.90 mM; ultrasonic and warming and heat to 60°C)
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.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 5 mg/mL (20.90 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 5 mg/mL (20.90 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation
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Fiche technique (279 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Shimamoto K, et al. DL-threo-beta-benzyloxyaspartate, a potent blocker of excitatory amino acid transporters. Mol Pharmacol. 1998 Feb;53(2):195-201. [Content Brief]
[2]. Jabaudon D, et al. Inhibition of uptake unmasks rapid extracellular turnover of glutamate of nonvesicular origin. Proc Natl Acad Sci U S A. 1999 Jul 20;96(15):8733-8. [Content Brief]
[3]. Shigeri Y, et al. Effects of threo-beta-hydroxyaspartate derivatives on excitatory amino acid transporters (EAAT4 and EAAT5). J Neurochem. 2001 Oct;79(2):297-302. [Content Brief]
[4]. Pedraz-Cuesta E, et al. The glutamate transport inhibitor DL-Threo-β-Benzyloxyaspartic acid (DL-TBOA) differentially affects SN38- and oxaliplatin-induced death of drug-resistant colorectal cancer cells. BMC Cancer. 2015 May 16;15:411. [Content Brief]
[5]. Yumiko Sekiya, et al. Facilitation of morphine withdrawal symptoms and morphine-induced conditioned place preference by a glutamate transporter inhibitor DL-threo-beta-benzyloxyaspartate in rats. Eur J Pharmacol. 2004 Feb 6;485(1-3):201-10. [Content Brief]
Complete Stock Solution Preparation Table
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.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 4.1801 mL | 20.9004 mL | 41.8008 mL | 104.5019 mL |
| 5 mM | 0.8360 mL | 4.1801 mL | 8.3602 mL | 20.9004 mL | |
| 10 mM | 0.4180 mL | 2.0900 mL | 4.1801 mL | 10.4502 mL | |
| 15 mM | 0.2787 mL | 1.3934 mL | 2.7867 mL | 6.9668 mL | |
| 20 mM | 0.2090 mL | 1.0450 mL | 2.0900 mL | 5.2251 mL | |
| DMSO | 25 mM | 0.1672 mL | 0.8360 mL | 1.6720 mL | 4.1801 mL |
| 30 mM | 0.1393 mL | 0.6967 mL | 1.3934 mL | 3.4834 mL | |
| 40 mM | 0.1045 mL | 0.5225 mL | 1.0450 mL | 2.6125 mL | |
| 50 mM | 0.0836 mL | 0.4180 mL | 0.8360 mL | 2.0900 mL | |
| 60 mM | 0.0697 mL | 0.3483 mL | 0.6967 mL | 1.7417 mL | |
| 80 mM | 0.0523 mL | 0.2613 mL | 0.5225 mL | 1.3063 mL | |
| 100 mM | 0.0418 mL | 0.2090 mL | 0.4180 mL | 1.0450 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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