GATT-44 

GATT-44 is a blood-brain barrier-permeable, selective GABA transporter 1 (GAT-1) ligand with an IC₅₀ of 126 nM. GATT-44 shows selectivity for GAT-2, GAT-3 and BGT-1 subtypes, and undergoes copper-mediated ¹⁸F-radiofluorination. The radiolabeled GATT-44 ([¹⁸F]GATT-44) exhibits brain uptake, metabolic stability and high GAT-1 binding specificity in non-human primates. GATT-44 is applicable for research on neurodegenerative and neuropsychiatric diseases^[1].

GATT-44 potently inhibits GAT-1 binding in rat brain slices with an IC₅₀ of <100 nM^[1].
GATT-44 (50 μM) selectively inhibits GAT-1 in transfected cells with an IC₅₀ of 126 nM, with no activity against GAT-2, GAT-3, or BGT-1^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

[¹⁸F]GATT-44 (administered via slow intravenous bolus over 3 min) exhibits favorable brain penetration, slow plasma metabolism rate, and specific GAT-1 binding capacity in rhesus monkeys, with its regional BP_nD values consistent with the expression levels of endogenous GAT-1^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

367.46

C₂₃H₂₆FNO₂

1265900-99-9

FC1=C(/C(C2=CC=CC=C2C)=C/CCN3C[C@@H](CCC3)C(O)=O)C=CC=C1

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Gu J, et al. Discovery of the First Brain-Penetrant Radioligands for Visualizing the GABA Transporter 1 (GAT-1): Synthesis, In Vitro Screening, and In Vivo Evaluation in Nonhuman Primates. J Med Chem. Published online April 7, 2026.