S44819

Research use only, not for human use.

S44819 (S-44819, Egis-1352 Afizagabar) is a novel potent, competitive, selective antagonist of the α5-GABAAR with Kd of 221 nM, IC50 of 585 nM (α5β2γ2).

S44819 (S-44819, Egis-1352 Afizagabar) is a novel potent, competitive, selective antagonist of the α5-GABAAR with Kd of 221 nM, IC50 of 585 nM (α5β2γ2); does not inhibit the activation of α5-GABAARs by etomidate, displays week activity against α1β2γ2 (IC50=2.4 uM) and α3β2γ2 (IC50=3.7 uM); enhances hippocampal synaptic plasticity and exhibits pro-cognitive efficacy in vivo.Stroke Phase 2 Clinical.

Afizagabar (S44819) is a competitive α5-GABAAR antagonist (Kb=221 nM). Afizagabar selectively inhibits extrasynaptic α5-GABAARs of mouse CA1 pyramidal neurons.

Afizagabar (1 and 3 mg/kg; i.p.) significantly diminishes the marked increase in total errors induced by Scopolamine. Animal Model:Male Sprague Dawley (SPRD) rats (In the eight-arm radial maze)Dosage:1 and 3 mg/kg Administration:I.p. Result:Significantly diminished the marked increase in total errors induced by Scopolamine.

S-44819 | Egis-13529 | Afizagabar

Membrane Transporter/Ion Channel

iGluR

iGluR

Neurological Disease

Stroke

1398496-82-6

365.382

C19H12FN3O2S

>98% (HPLC)

In Vitro:?DMSO : 6.25 mg/mL (17.11 mM)

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

5-(4-Fluoro-1-benzothiophen-2-yl)-8-methyl-1,9-dihydro2H-[1,3]oxazolo[4,5-H][2,3]benzodiazepin-2-one

(-20℃)

With Ice Pack

≥ 2 years