GABAA receptor agent 2 (TFA)

GABAA receptor agent 2 (TFA)

• CAS Number: 1781880-44-1
• UNSPSC Description: 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 Antigen: GABA Receptor
• Type: Reference compound
• Related Pathways: Membrane Transporter/Ion Channel;Neuronal Signaling
• Applications: Neuroscience-Neuromodulation
• Field of Research: Neurological Disease
• Assay Protocol: https://www.medchemexpress.com/gabaa-receptor-agent-2-tfa.html
• Solubility: 10 mM in DMSO
• Smiles: ON1N=CC(C2CCNCC2)=C1C3=CC(C4=CC=CC=C4)=CC=C3.OC(C(F)(F)F)=O
• Molecular Weight: 433.42
• References & Citations: [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.
• Shipping Conditions: Room temperature
• Clinical Information: No Development Reported