Afizagabar
Based on 2 publication(s) in Google Scholar
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.
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- Reinheit: 98.40%
- CAS. Nr.: 1398496-82-6
- Formel: C19H12FN3O2S
- Molecular Weight:365.38
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Afizagabar
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Biologische Aktivität
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Sprague Dawley (SPRD) rats (In the eight-arm radial maze)[1]
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Dosage:1 and 3 mg/kg
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Administration:I.p.
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Result:Significantly diminished the marked increase in total errors induced by Scopolamine.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 1398496-82-6
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Appearance Solid
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Molecular Weight 365.38
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Formel C19H12FN3O2S
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Color Light yellow to yellow
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SMILES
O=C(N1)OC2=C1C=C3CC(C)=NN=C(C4=CC5=C(F)C=CC=C5S4)C3=C2
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Synonyms
S44819; Egis-13529
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (2)
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Journal Impact Factor
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Most Recent
Lösungsmittel & Löslichkeit
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)
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.
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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Reinheit & Dokumentation
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Data Sheet (282 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
Verweise
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 |
Afizagabar Related Classifications
HY-120051 Related Classifications
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