产品描述
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].
体外活性
Afizagabar (S44819) is a competitive α5-GABAAR antagonist (Kb=221 nM). Afizagabar selectively inhibits extrasynaptic α5-GABAARs of mouse CA1 pyramidal neurons[1].
体内活性
Afizagabar (1 and 3 mg/kg; i.p.) significantly diminishes the marked increase in total errors induced by Scopolamine[1].
Cas No.
1398496-82-6
分子式
C19H12FN3O2S
分子量
365.38
别名
Afizagabar
储存和溶解度
DMSO:6.25 mg/mL (17.11 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years