[CAS NO. 480439-73-4] TFB-TBOA
PRODUCTS SPECIFICATIONS [480439-73-4]
DESCRIPTION [480439-73-4]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 426.34 |
| Molecular Formula | C19H17F3N2O6 |
| SMILES | O=C(C1=CC=C(C=C1)C(F)(F)F)NC2=CC(CO[C@H](C(O)=O)[C@H](N)C(O)=O)=CC=C2 |
Summary
TFB-TBOA (CF3-Bza-TBOA) is a potent glutamate transporter blocker that potently suppresses the activity of glial transporters. TFB-TBOA shows IC 50 values of 22, 17, and 300 nM for glutamate transporters EAAT1, EAAT2 , and EAAT3 respectively in an uptake assay using cells transiently expressing EAATs [1] .
In Vitro
TFB-TBOA (CF3-Bza-TBOA) inhibits synaptically activated transporter currents (STCs) in astrocytes in the stratum radiatum in rat hippocampal slices in a dose-dependent manner with an IC
50
of 13 nM, and reduces them to approximately 10% of the control at 100 nM
[2]
.
TFB-TBOA inhibits the Na
+
i
response evoked by 200 µM glutamate in a concentration-dependent manner with IC
50
value of 43 nM, as measured on the amplitude of the Na
+
i
response
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 50 mg/mL ( 117.28 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 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 |
References
- [1] Shimamoto K, et al. Characterization of novel L-threo-beta-benzyloxyaspartate derivatives, potent blockers of the glutamate transporters. Mol Pharmacol. 2004;65(4):1008-1015.
- [2] Tsukada S, et al. 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] Bozzo L, et al. 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.