GABAA receptor agent 2 TFA
GABAA receptor agent 2 TFA is a potent and high-affinity GABAA receptor antagonist with an IC50 of 24 nM (human α1β2γ2 GABAA-expressing tsA201 cells) and a Ki of 28 nM (rat GABAA receptors). GABAA receptor agent 2 TFA is inactive against four human GABA transporters (hGAT-1, hBGT-1, hGAT-2, and hGAT-3).
For research use only. We do not sell to patients.
- CAS No.: 1781880-44-1
- Formula: C22H22F3N3O3
- Molecular Weight:433.42
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
IC50: 24 nM (Human α1β2γ2 GABAA-expressing tsA201 cells)[1]
Ki: 28 nM (Rat GABAA receptors)[1]
With the protonated piperidine nitrogen consistently placed to interact with β2 E155, only a simultaneous interaction with α1 R66 provided enough space above and below the ligand heteroaromatic ring to be compatible with the high affinity (0.022 μM) of the disubstituted GABAA receptor agent 2 (compound 19)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1781880-44-1
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Molecular Weight 433.42
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Formula C22H22F3N3O3
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SMILES
ON1N=CC(C2CCNCC2)=C1C3=CC(C4=CC=CC=C4)=CC=C3.OC(C(F)(F)F)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[1]. Henriette A Møller, et al. Novel 4-(piperidin-4-yl)-1-hydroxypyrazoles as gamma-aminobutyric acid(A) receptor ligands: synthesis, pharmacology, and structure-activity relationships. J Med Chem. 2010 Apr 22;53(8):3417-21. [Content Brief]
[2]. Tommy Sander, et al. New insights into the GABA(A) receptor structure and orthosteric ligand binding: receptor modeling guided by experimental data. Proteins. 2011 May;79(5):1458-77. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
GABAA receptor agent 2 TFA Related Classifications
HY-135482 Related Classifications
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