1. GPCR/G Protein
    Neuronal Signaling
  2. 5-HT Receptor
  3. AVN-492

AVN-492 

Cat. No.: HY-101924 Purity: 99.49%
Handling Instructions

AVN-492 is a very specific and highly-selective antagonist with picomolar affinity to 5-HT6R (Ki=91 pM).

For research use only. We do not sell to patients.

AVN-492 Chemical Structure

AVN-492 Chemical Structure

CAS No. : 1220646-23-0

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Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 71 In-stock
Estimated Time of Arrival: December 31
5 mg USD 90 In-stock
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10 mg USD 150 In-stock
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25 mg USD 300 In-stock
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50 mg USD 450 In-stock
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100 mg USD 650 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

AVN-492 is a very specific and highly-selective antagonist with picomolar affinity to 5-HT6R (Ki=91 pM).

IC50 & Target

5-HT6 Receptor

91 pM (Ki)

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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

359.45

Formula

C₁₇H₂₁N₅O₂S

CAS No.

1220646-23-0

SMILES

O=S(C1=CC=CC=C1)(C2=C3N(C(C)=C(N(C)C)C(C)=N3)N=C2NC)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (278.20 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7820 mL 13.9101 mL 27.8203 mL
5 mM 0.5564 mL 2.7820 mL 5.5641 mL
10 mM 0.2782 mL 1.3910 mL 2.7820 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Animal Administration
[1]

Mice and Rats[1]
For pharmacokinetic, behavior, and toxicity studies, male Wistar rats (220-242 g), male CD1 mice (24-30 g), male SHK mice (20-25 g), and male Balb/C mice (15-20 g) are used. The pharmacokinetic profiling of AVN-492 is performed on male CD-1 mice and male Wistar rats. Each dose-route group of rodents consist of 3 animals. AVN-492 is administered either intravenously (IV) or orally (PO). At different time points after the drug administration, the animals are quickly euthanized by placing them into CO2 chamber. Blood samples are drawn through a cardiopuncture. In separate experiments, AVN-492 is orally administered to male Wistar rats at doses of 1 mg/kg, 3 mg/kg, and 10 mg/kg (3 independent groups, 3 animals per group). The animals are anesthetized 60 min later with 5% halothane, positioned in a stereotaxic frame, and samples of cerebrospinal fluid (CSF) are taken through 23G needle from the cisterna magna. CSF samples are checked for the absence of blood contamination. After the CSF samples are taken, the blood samples are drawn through a cardiopuncture and the brains are removed, washed immediately with ice-cold saline, and homogenized in a 1:4 brain tissue/water mixture. AVN-492 is extracted from all the samples with acetonitrile and concentrations are determined.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

Purity: 99.49%

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Keywords:

AVN-492AVN492AVN 4925-HT ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorInhibitorinhibitorinhibit

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