| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| Other Sizes |
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| Targets |
EAAT1 EAAT2 EAAT3
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|---|---|
| ln Vitro |
DL-TBOA treatment (70-350 μM; 48 hours; HCT116 and LoVo cell lines) increased the viability loss induced by SN38 in a concentration-dependent manner. Oxaliplatin-induced loss of viability is reversed by DL-TBOA [4]. HCT116 and LoVo cell lines treated with DL-TBOA (350 μM; 24 hours) show a reduction in p53 induction caused by SN38 and Oxaliplatin [4].
|
| ln Vivo |
The manifestation of Naloxone-induced somatic symptoms and conditioned location aversion is markedly enhanced by DL-TBOA (10 nmol; icv, rat)[5].
|
| Cell Assay |
Cell Viability Assay[4]
Cell Types: HCT116 and LoVo cell lines Tested Tested Concentrations: 70 μM, 350 μM Incubation Duration: 48 hrs (hours) Experimental Results: Enhanced SN38-induced, and counteracted Oxaliplatin-induced, cell death. Cell Viability Assay[4] Cell Types: HCT116 and LoVo cell lines Tested Tested Concentrations: 350 μM Incubation Duration: 24 hrs (hours) Experimental Results: p53 induction by SN38 and oxaliplatin was decreased. |
| Animal Protocol |
Animal/Disease Models: Male SD (Sprague-Dawley) rats (180-250 g)[5]
Doses: 1 nmol, 3 nmol, 10 nmol Route of Administration: Intracerebroventricular injection (icv) Experimental Results: Dose dependently facilitated various somatic signs induced by Naloxone (0.1 mg/kg ). |
| References |
[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.
[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. [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. [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. [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. |
| Molecular Formula |
C11H13NO5
|
|---|---|
| Molecular Weight |
239.23
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| CAS # |
205309-81-5
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| Related CAS # |
DL-TBOA ammonium;2093503-71-8
|
| SMILES |
O(CC1C=CC=CC=1)C(C(=O)O)C(C(=O)O)N
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| Solubility (In Vitro) |
DMSO: 200 mg/mL (836.02 mM)
H2O: 5 mg/mL (20.90 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5 mg/mL (20.90 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 50.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 5 mg/mL (20.90 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 50.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 5 mg/mL (20.90 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.1801 mL | 20.9004 mL | 41.8008 mL | |
| 5 mM | 0.8360 mL | 4.1801 mL | 8.3602 mL | |
| 10 mM | 0.4180 mL | 2.0900 mL | 4.1801 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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