GABAA receptor agent 2 TFA_product_DataBase

Bioactivity	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)[1].
Target	IC50: 24 nM (Human α1β2γ2 GABAA-expressing tsA201 cells)Ki: 28 nM (Rat GABAA receptors)
Invitro	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].
Name	GABAA receptor agent 2 TFA
CAS	1781880-44-1
Formula	C22H22F3N3O3
Molar Mass	433.42
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[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. [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.

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