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Afizagabar

Catalog No. T37388Cas No. 1398496-82-6

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].

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Pack Size	Price	Availability
25 mg	$1,900	8-10 weeks
50 mg	$2,480	8-10 weeks
100 mg	$3,400	8-10 weeks

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Product Introduction

Bioactivity

Description	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]. Afizagabar (S44819) is a competitive α5-GABAAR antagonist (Kb=221 nM). Afizagabar selectively inhibits extrasynaptic α5-GABAARs of mouse CA1 pyramidal neurons[1]. Afizagabar (1 and 3 mg/kg; i.p.) significantly diminishes the marked increase in total errors induced by Scopolamine[1]. [1]. Etherington LA, et al. Selective inhibition of extra-synaptic α5-GABAA receptors by S44819, a new therapeutic agent. Neuropharmacology. 2017;125:353-364.
In vitro	Afizagabar (S44819) is a competitive α5-GABAAR antagonist (Kb=221 nM). Afizagabar selectively inhibits extrasynaptic α5-GABAARs of mouse CA1 pyramidal neurons[1].
In vivo	Afizagabar (1 and 3 mg/kg; i.p.) significantly diminishes the marked increase in total errors induced by Scopolamine[1].

Chemical Properties

Molecular Weight	365.38
Formula	C19H12FN3O2S
Cas No.	1398496-82-6

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 6.25 mg/mL (17.11 mM)

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.7369 mL	13.6844 mL	27.3688 mL	136.8438 mL
5 mM	0.5474 mL	2.7369 mL	5.4738 mL	27.3688 mL
10 mM	0.2737 mL	1.3684 mL	2.7369 mL	13.6844 mL

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DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

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Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O TargetMol | reagent

mix well and clarify

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