AVN-492
AVN-492 Basic information
- Product Name:
- AVN-492
- Synonyms:
-
- AVN-492
- AVN-492; AVN 492; AVN492;1220646-23-0
- CS-2812
- Pyrazolo[1,5-a]pyrimidine-2,6-diamine, N2,N6,N6,5,7-pentamethyl-3-(phenylsulfonyl)-
- N2,N6,N6,5,7-Pentamethyl-3-(phenylsulfonyl)pyrazolo[1,5-a]pyrimidine-2,6-diamine
- inhibit,5-HT Receptor,Inhibitor,AVN-492,Serotonin Receptor,AVN 492,5-hydroxytryptamine Receptor
- 3-(benzenesulfonyl)-N2,5,N6,N6,7-pentamethylpyrazolo[1,5-a]pyrimidine-2,6-diamine
- AVN-492, 10 mM in DMSO
- CAS:
- 1220646-23-0
- MF:
- C17H21N5O2S
- MW:
- 359.45
- Product Categories:
-
- API
- Mol File:
- 1220646-23-0.mol
AVN-492 Chemical Properties
- Density
- 1.31±0.1 g/cm3(Predicted)
- storage temp.
- Keep in dark place,Sealed in dry,Store in freezer, under -20°C
- solubility
- DMSO:62.5(Max Conc. mg/mL);173.88(Max Conc. mM)
DMF:25.0(Max Conc. mg/mL);69.55(Max Conc. mM)
DMF:PBS (pH 7.2) (1:20):0.04(Max Conc. mg/mL);0.11(Max Conc. mM)
Ethanol:1.0(Max Conc. mg/mL);2.78(Max Conc. mM) - form
- A crystalline solid
- pka
- 1.04±0.30(Predicted)
- color
- White to light yellow
AVN-492 Usage And Synthesis
Uses
AVN-492 is a very specific and highly-selective antagonist with picomolar affinity to 5-HT6R (Ki=91 pM).
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 10mg/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[1].
IC 50
5-HT6 Receptor: 91 pM (Ki)
References
[1] Ivachtchenko AV, et al. AVN-492, A Novel Highly Selective 5-HT6R Antagonist: Preclinical Evaluation. J Alzheimers Dis. 2017;58(4):1043-1063. DOI:10.3233/JAD-161262
AVN-492Supplier
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