TFB-TBOA (CF3-Bza-TBOA) is a potent glutamate transporter blocker that potently suppresses the activity of glial transporters. TFB-TBOA shows IC50 values of 22, 17, and 300 nM for glutamate transporters EAAT1, EAAT2, and EAAT3 respectively in an uptake assay using cells transiently expressing EAATs.
| Molecular Weight | 426.34 |
| Formula | C19H17F3N2O6 |
| CAS Number | 480439-73-4 |
| Form | Solid |
| Solubility (25°C) | DMSO 50 mg/mL (ultrasonic) |
| Storage | Powder -20°C |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related EAAT Products |
|---|
| cis-α-(Carboxycyclopropyl)glycine
cis-α-(Carboxycyclopropyl)glycine (L-CCG III) is a potent, competitive glutamate uptake inhibitor. |
| Troriluzole Hydrochloride
Troriluzole Hydrochloride is the hydrochloride form of Troriluzole, and is also an excitatory amino acid transporter protein 2 (EAAT2) modulator, which increases glutamate uptake at neuronal synapses by increasing the expression of EAAT in neuroglia and enhancing its function, thereby decreasing glutamate levels in neuronal synapses. It can be used in studies related to spinocerebellar ataxia (SCA) and anxiety disorders. |
| Trigriluzole
Trigriluzole is an excitatory amino acid transporter protein 2 (EAAT2) modulator that increases the uptake of glutamate at neuronal synapses by increasing the expression and enhancing the function of EAAT in glial cells, thereby decreasing glutamate levels in neuronal synapses. It can be used in studies related to spinocerebellar ataxia (SCA) and anxiety disorders. |
| GT 949
GT 949 is a selective excitatory amino acid transporter-2 (EAAT2) positive allosteric modulator with an EC50 of 0.26 nM. |
| WAY-213613 hydrochloride
WAY-213613 hydrochloride is a potent, selective nonsubstrate reuptake inhibitor of GLT-1/EAAT2 with IC50 of 85 nM EAAT2. |
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