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Afizagabar

Cat. No. M21509
Afizagabar Structure
Synonym:

S44819; Egis-13529

Size Price Availability
5mg USD 500  USD500 1-2 Weeks
10mg USD 850  USD850 1-2 Weeks
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Quality Control & Documentation
Biological Activity

Afizagabar (S44819) is a first-in-class, competitive and selective α5-GABAAR antagonist with an IC50 value of 585 nM for α5β2γ2 and a Ki of 66 nM for α5β3γ2.

Chemical Information
Molecular Weight 365.38
Formula C19H12FN3O2S
CAS Number 1398496-82-6
Solubility (25°C) DMSO : 6.25 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

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Keywords: Afizagabar, S44819; Egis-13529 supplier, GABA Receptor, inhibitors, activators


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