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

AVN-492 

目录号: HY-101924 纯度: 99.49%
产品使用指南

AVN-492 是一种高特异性的选择性 5-HT6R 拮抗剂,对 5-HT6R 具有皮摩尔级亲和力,Ki 为 91 pM。

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AVN-492 Chemical Structure

AVN-492 Chemical Structure

CAS No. : 1220646-23-0

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生物活性

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)

体外研究
(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.

体内研究
(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.

分子量

359.45

Formula

C17H21N5O2S

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 100 mg/mL (278.20 mM)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 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
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

参考文献
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.

参考文献

纯度: 99.49%

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2

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产品名称:
AVN-492
目录号:
HY-101924
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