Afizagabar (C09-1102-639)

Afizagabar (S44819) is a first-in-class, competitive, and selective antagonist at the GABA-binding site of the α5-GABAAR , with an IC 50 of 585 nM for α5β2γ2 and a K i of 66 nM for α5β3γ2. Afizagabar enhances hippocampal synaptic plasticity and exhibits pro-cognitive efficacy.In VitroAfizagabar (S44819) is a competitive α5-GABAAR antagonist (K b =221 nM). Afizagabar selectively inhibits extrasynaptic α5-GABAARs of mouse CA1 pyramidal neurons. MCE has not independently confirmed the accuracy of these methods. They are for reference only.In VivoAfizagabar (1 and 3 mg/kg; i.p.) significantly diminishes the marked increase in total errors induced by Scopolamine . MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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.Form:Solid. Specifications and Purity: 98%. Molecular Formula: C19H12FN3O2S. Molecular Weight: 365.38. PubChem CID: 136209703. Isomeric SMILES: CC1=NN=C(C2=CC3=C(C=C2C1)NC(=O)O3)C4=CC5=C(C=CC=C5S4)F.