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

Afizagabar  (Synonyms: S44819; Egis-13529)

Cat. No.: HY-120051 Purity: 98.29%
COA 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
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 550 In-stock
Solution
10 mM * 1 mL in DMSO USD 550 In-stock
Solid
5 mg USD 500 In-stock
10 mg USD 850 In-stock
25 mg USD 1800 In-stock
50 mg USD 3000 In-stock
100 mg USD 4600 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

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  • Biological Activity

  • Purity & Documentation

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  • Customer Review

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].

MedChemExpress (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].

MedChemExpress (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.
Clinical Trial
Molecular Weight

365.38

Formula

C19H12FN3O2S

CAS No.
Appearance

Solid

Color

Light yellow to yellow

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 : 6.25 mg/mL (17.11 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 98.29%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.7369 mL 13.6844 mL 27.3688 mL 68.4219 mL
5 mM 0.5474 mL 2.7369 mL 5.4738 mL 13.6844 mL
10 mM 0.2737 mL 1.3684 mL 2.7369 mL 6.8422 mL
15 mM 0.1825 mL 0.9123 mL 1.8246 mL 4.5615 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
Afizagabar
Cat. No.:
HY-120051
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