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Art. -Nr.: 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.

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CAS. Nr.: 1265900-99-9
Formel: C₂₃H₂₆FNO₂
Molecular Weight:367.46

Speicherung:

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

GATT-44 Chemical Structure

CAS. Nr.: 1265900-99-9

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Use of MCE Products

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

Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
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Biologische Aktivität

Beschreibung

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. Nr. 1265900-99-9
Molecular Weight 367.46
Formel C₂₃H₂₆FNO₂
SMILES

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

Room temperature in continental US; may vary elsewhere.
Speicherung

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

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[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]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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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100 mg

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