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AVN-492

Cat. No. M9763
AVN-492 Structure
Size Price Availability
10mg USD 160  USD160 4-7 Days
25mg USD 320  USD320 4-7 Days
50mg USD 480  USD480 4-7 Days
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

AVN-492 is a potent and selective 5-HT6R antagonist, binds to 5-HT6R (Ki = 91 pM). AVN-492 displays great 5-HT6R selectivity against all other serotonin receptor subtypes, and is extremely specific against any other receptors such as adrenergic, GABAergic, dopaminergic, histaminergic, etc. In mice, the plasma and brain concentrations of AVN-492, given IV at a dose of 2 mg/kg, decreased with time but at both time points, 15 min and 60 min, the brain/plasma ratio (mean±SEM) is nearly the same, at 13.2±0.7% and 9.0±1.5%, respectively.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 359.45
Formula C17H21N5O2S
CAS Number 1220646-23-0
Purity >99%
Solubility DMSO ≥ 75 mg/mL
Storage at -20°C
References

[1] Alexandre V Ivachtchenko, et al. J Alzheimers Dis. AVN-492, A Novel Highly Selective 5-HT6R Antagonist: Preclinical Evaluation

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