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.
Product information
CAS Number: 1398496-82-6
Molecular Weight: 365.38
Formula: C19H12FN3O2S
Chemical Name: 10-(4-fluoro-1-benzothiophen-2-yl)-13-methyl-6-oxa-4,11,12-triazatricyclo[7.5.0.0³,⁷]tetradeca-1,3(7),8,10,12-pentaen-5-one
Smiles: CC1CC2=CC3NC(=O)OC=3C=C2C(=NN=1)C1=CC2=C(F)C=CC=C2S1
InChiKey: WNUWGRVHGICCLS-UHFFFAOYSA-N
InChi: InChI=1S/C19H12FN3O2S/c1-9-5-10-6-14-15(25-19(24)21-14)7-11(10)18(23-22-9)17-8-12-13(20)3-2-4-16(12)26-17/h2-4,6-8H,5H2,1H3,(H,21,24)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 6.25 mg/mL (17.11 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
Afizagabar (S44819) is a competitive α5-GABAAR antagonist (Kb=221 nM). Afizagabar selectively inhibits extrasynaptic α5-GABAARs of mouse CA1 pyramidal neurons.
In Vivo:
Afizagabar (1 and 3 mg/kg; i.p.) significantly diminishes the marked increase in total errors induced by Scopolamine.
Products are for research use only. Not for human use.
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