AVN492

SKU: orb1221173

Description

AVN-492 is a potent and selective 5-HT6R Antagonist (Ki: 91 pM).

Key Properties

• CAS Number: 1220646-23-0
• MW: 359.45
• Purity: >98% (HPLC)
• Formula: C₁₇H₂₁N₅O₂S
• SMILES: CNc1nn2c(C)c(N(C)C)c(C)nc2c1S(=O)(=O)c1ccccc1
• Target: 5-HT Receptor
• Solubility: DMSO: 100 mg/mL

Bioactivity

• In Vivo:
  In rats, the plasma, brain, and CSF concentrations of the PO administered AVN-492 are dose-dependent. The drug concentration curves for the plasma and brain are of hyperbolic shape and at all doses the brain-plasma ratio is near 11%. The drug concentration in CSF, however, is nearly linearly dependent on the dose, reaching 50% of the plasma level at 10 mg/kg. 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. This indicates that the steady-state concentration gradient of AVN-492 is established by at least 15 min after the drug administration.
• In Vitro:
  The affinity of AVN-492 to bind to 5-HT6R (Ki=91 pM) is more than three orders of magnitude higher than that to bind to the only other target, 5-HT2BR, (Ki=170 nM). Thus, 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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

5-HT Receptor