EAAT1 Inhibitor

DL-TBOA is a potent non-transportable inhibitor of excitatory amino acid transporters with IC₅₀s of 70 μM, 6 μM and 6 μM for excitatory amino acid transporter-1 (EAAT1), EAAT2 and EAAT3, respectively. DL-TBOA inhibits the uptake of [¹⁴C]glutamate in COS-1 cells expressing the human EAAT1 and EAAT2 with K_i valuesof 42 μM and 5.7 μM, respectively. DL-TBOA blocks EAAT4 and EAAT5 in a competitive manner with K_i values of 4.4 μM and 3.2 μM, respectively.

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.

SN05 is a potent amino acid transport (AAT) inhibitor with K_i values of 2.77 μM, 0.73 μM, 0.87 μM, 3.7 μM, 7.25 μM, 7.23 μM and 2.22 μM for hASCT1, rASCT2, hASCT2, EAAT1, EAAT2, EAAC1 and EAAT5, respectively. SN05 can be used in the study of cancer.

SLC1A1/EAAT3-IN-1 (Compound 3e) is a selective EAAT3 inhibitor with an IC₅₀ of 7.2  μM for hEAAT3 over EAAT1,2,4 (IC₅₀: ∼ 250 μM). SLC1A1/EAAT3-IN-1 can be used for psychiatric disorders such as obsessive compulsive disorder and schizophrenia research.

SN40 is a potent amino acid transport (AAT) inhibitor with K_is of 7.29 μM, 2.42 μM, 2.94 μM, 5.55 μM, 24.43 μM and 5.55 μM for rat ASCT2, human ASCT2, EAAT1, EAAT2, EAAC1 and EAAT5, respectively. SN40 can be used for researching anticancer.

DL-TBOA ammonium is a potent non-transportable inhibitor of excitatory amino acid transporters with IC₅₀s of 70 μM, 6 μM and 6 μM for excitatory amino acid transporter-1 (EAAT1), EAAT2 and EAAT3, respectively. DL-TBOA ammonium inhibits the uptake of [¹⁴C]glutamate in COS-1 cells expressing the human EAAT1 and EAAT2 with K_i valuesof 42 μM and 5.7 μM, respectively. DL-TBOA ammonium blocks EAAT4 and EAAT5 in a competitive manner with K_i values of 4.4 μM and 3.2 μM, respectively.