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TFB-TBOA (CF3-Bza-TBOA)

Cat No.:V74187 Purity: ≥98%
TFB-TBOA (CF3-Bza-TBOA) is a potent glutamate transporter blocker that can effectively inhibit the activity of glial transporters.
TFB-TBOA (CF3-Bza-TBOA)
TFB-TBOA (CF3-Bza-TBOA) Chemical Structure CAS No.: 480439-73-4
Product category: EAAT
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
1mg
5mg
Other Sizes
Official Supplier of:
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Product Description
TFB-TBOA (CF3-Bza-TBOA) is a potent glutamate transporter blocker that can effectively inhibit the activity of glial transporters. The IC50s of TFB-TBOA for glutamate transporters EAAT1, EAAT2, and EAAT3 are 22, 17, and 300 nM, respectively.
Biological Activity I Assay Protocols (From Reference)
Targets
EAAT1 EAAT2 EAAT3
ln Vitro
TFB-TBOA (CF3-Bza-TBOA) lowers synaptically activated transporter currents (STCs) to about 10% of the control at 100 nM. It does this in a dose-dependent manner in astrocytes in the stratum radiatum in rat hippocampus slices, with an IC50 of 13 nM[2]. Based on the amplitude of the Na+i response, TFB-TBOA exhibits concentration-dependent inhibition of the Na+i response elicited by 200 µM glutamate, with an IC50 value of 43 nM[1].
References

[1]. Characterization of novel L-threo-beta-benzyloxyaspartate derivatives, potent blockers of the glutamate transporters. Mol Pharmacol. 2004;65(4):1008-1015.

[2]. Effects of a novel glutamate transporter blocker, (2S, 3S)-3-[3-[4-(trifluoromethyl)benzoylamino]benzyloxy]aspartate (TFB-TBOA), on activities of hippocampal neurons. Neuropharmacology. 2005;48(4):479-491.

[3]. Inhibitory effects of (2S, 3S)-3-[3-[4-(trifluoromethyl)benzoylamino]benzyloxy]aspartate (TFB-TBOA) on the astrocytic sodium responses to glutamate. Brain Res. 2010;1316:27-34.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C19H17F3N2O6
Molecular Weight
426.34
Exact Mass
426.104
CAS #
480439-73-4
PubChem CID
52941382
Appearance
White to off-white solid powder
LogP
3.112
Hydrogen Bond Donor Count
4
Hydrogen Bond Acceptor Count
10
Rotatable Bond Count
8
Heavy Atom Count
30
Complexity
622
Defined Atom Stereocenter Count
2
SMILES
C1=CC(=CC(=C1)NC(=O)C2=CC=C(C=C2)C(F)(F)F)CO[C@@H]([C@@H](C(=O)O)N)C(=O)O
InChi Key
LPWONNPEPDHEAI-GJZGRUSLSA-N
InChi Code
InChI=1S/C19H17F3N2O6/c20-19(21,22)12-6-4-11(5-7-12)16(25)24-13-3-1-2-10(8-13)9-30-15(18(28)29)14(23)17(26)27/h1-8,14-15H,9,23H2,(H,24,25)(H,26,27)(H,28,29)/t14-,15-/m0/s1
Chemical Name
(2S,3S)-2-amino-3-[[3-[[4-(trifluoromethyl)benzoyl]amino]phenyl]methoxy]butanedioic acid
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 Data
Solubility (In Vitro)
DMSO: 50 mg/mL (117.28 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 1.25 mg/mL (2.93 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 12.5 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: ≥ 1.25 mg/mL (2.93 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 12.5 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.

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Solubility in Formulation 3: ≥ 1.25 mg/mL (2.93 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 12.5 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.


 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.3455 mL 11.7277 mL 23.4555 mL
5 mM 0.4691 mL 2.3455 mL 4.6911 mL
10 mM 0.2346 mL 1.1728 mL 2.3455 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.

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What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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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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