1. Membrane Transporter/Ion Channel
    Neuronal Signaling
  2. GABA Receptor
  3. Afizagabar

Afizagabar (Synonyms: S44819; Egis-13529)

Cat. No.: HY-120051 Purity: 98.14%
Handling Instructions

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.

For research use only. We do not sell to patients.

Afizagabar Chemical Structure

Afizagabar Chemical Structure

CAS No. : 1398496-82-6

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 550 In-stock
Estimated Time of Arrival: December 31
5 mg USD 500 In-stock
Estimated Time of Arrival: December 31
10 mg USD 850 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1800 In-stock
Estimated Time of Arrival: December 31
50 mg USD 3000 In-stock
Estimated Time of Arrival: December 31
100 mg USD 4600 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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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].

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Afizagabar (1 and 3 mg/kg; i.p.) significantly diminishes the marked increase in total errors induced by Scopolamine[1].

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)[1]
Dosage: 1 and 3 mg/kg
Administration: I.p.
Result: Significantly diminished the marked increase in total errors induced by Scopolamine.
Molecular Weight

365.38

Formula

C₁₉H₁₂FN₃O₂S

CAS No.

1398496-82-6

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 10 mg/mL (27.37 mM; ultrasonic and warming and adjust pH to 10 with NaOH and heat to 80°C)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7369 mL 13.6844 mL 27.3688 mL
5 mM 0.5474 mL 2.7369 mL 5.4738 mL
10 mM 0.2737 mL 1.3684 mL 2.7369 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 1 mg/mL (2.74 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

AfizagabarS44819 Egis-13529S 44819S-44819Egis13529Egis 13529Egis-13529GABA ReceptorGamma-aminobutyric acid Receptorγ-Aminobutyric acid Receptorpro-cognitivehippocampalsynapticplasticitylearningInhibitorinhibitorinhibit

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Afizagabar
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HY-120051
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