T3MG is a selective inhibitor of excitatory amino acid transporters GLT-1, EAAT2, and EAAT4. T3MG has long been utilized as a gold standard in the study of general EAAT function. It has more recently been shown to be selective for EAAT2 and EAAT4 as compared to EAAT1 and EAAT3 in electrophysiology and glutamate/aspartate uptake assays. Although there are other EAAT2-selective compounds, this is the first tool with selectivity for EAAT4. T3MG is not a substrate for the transporters themselves, nor does it have activity at glutamate ion channels.
| Molecular Weight | 161.16 |
| Formula | C6H11NO4 |
| CAS Number | 63088-04-0 |
| Solubility (25°C) | Water: ≥1.5 mg/dL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| 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.
[3] M Sugawara, et al. Thyroid T4 5'-deiodinase activity in normal and abnormal human thyroid glands
[4] D Polk, et al. Nuclear thyroid hormone receptors: ontogeny and thyroid hormone effects in sheep
[5] J Beard, et al. Evidence for thyroid hormone deficiency in iron-deficient anemic rats
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