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Cat. No.: HY-182944

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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.

For research use only. We do not sell to patients.

CAS No.: 1265900-99-9
Formula: C₂₃H₂₆FNO₂
Molecular Weight:367.46

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

GATT-44 Chemical Structure

CAS No.: 1265900-99-9

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- In Vitro
- In Vivo
Chemical Information
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Biological Activity

Description

In Vitro

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.

In Vivo

[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.

Chemical Information

CAS No. 1265900-99-9
Molecular Weight 367.46
Formula C₂₃H₂₆FNO₂
SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage

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

Purity & Documentation

Handling Instructions (2659 KB)

References

[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. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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