Afizagabar

Afizagabar (S44819) is a first-in-class, competitive, and selective antagonist at the GABA-binding site of the α5-GABAAR, with an IC50 of 585 nM for α5β2γ2 and a Ki of 66 nM for α5β3γ2. Afizagabar enhances hippocampal synaptic plasticity and exhibits pro-cognitive efficacy[1].

Product Specifications

CAS Number

[1398496-82-6]

Product Name Alternative

S44819; Egis-13529

UNSPSC

12352005

Target

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/afizagabar.html

Concentration

10mM

Purity

98.40

Solubility

DMSO : 6.25 mg/mL (ultrasonic)

Smiles

O=C(N1)OC2=C1C=C3CC(C)=NN=C(C4=CC5=C(F)C=CC=C5S4)C3=C2

Molecular Formula

C19H12FN3O2S

Molecular Weight

365.38

References & Citations

[1]Etherington LA, et al. Selective inhibition of extra-synaptic α5-GABAA receptors by S44819, a new therapeutic agent. Neuropharmacology. 2017;125:353-364.