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AVN-492

产品编号 T5179 CAS 1220646-23-0

别名: AVN492

AVN-492 是一种有效的选择性 5-HT6R 拮抗剂，Ki 为 91 pM。

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AVN-492, CAS 1220646-23-0

规格	价格/CNY	货期
1 mg	￥ 786	现货
2 mg	￥ 1,180	现货
5 mg	￥ 1,970	现货
10 mg	￥ 2,970	现货
25 mg	￥ 4,890	现货
50 mg	￥ 6,860	现货
100 mg	￥ 9,450	现货
1 mL * 10 mM (in DMSO)	￥ 2,170	现货

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纯度: 99.29%

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	AVN-49 is a potent and selective 5-HT6R Antagonist (Ki: 91 pM).
靶点活性	5-HT6R:91 pM (Ki, cell free)
体外活性	Affinity of AVN-492, Ki^b, to compete with [3H]LSD for binding to 5-HT6R was estimated to be 91 pM (IC50^b = 194 pM). Affinity of 509 AVN-492 to the 5-HT2BR, Ki^b = 170 nM (IC50^b = 268 nM) was more than three orders of magnitude lower. Despite being metabolized by human microsomes, AVN-492 did not appreciably inhibit five major human recombinant CYP isoforms, CYP3A4, 1A2, 2C9, 2C19, and 2D6 at concentrations as high as 10 M [1].
体内活性	AVN-492 has high oral bioavailability and good brain permeability in rodents. In behavioral tests, AVN-492 shows an anxiolytic effect in the elevated plus-maze model, prevents an apomorphine-induced disruption of startle pre-pulse inhibition (the PPI model) and reverses scopolamine- and MK-801-induced memory deficit in passive avoidance model. No anti-obesity effect of AVN-492 was found in a murine model [1].
激酶实验	Assessment of AVN-492 selectivity was performed on a panel of 69 therapeutic targets including receptors, ion channels, neuromediator transporters, and enzymes. The full list of the targets is presented in the Supplementary Material. AVN-492 interactions with therapeutic targets were assessed by either equilibrium competitive displacement of corresponding radiolabeled ligands or inhibition of corresponding enzymatic activities. The studies were performed at Eurofins in accordance with their internally optimized procedures as briefly described in. The displacement of radioligands and inhibition of enzymatic activities were measured at AVN-492 concentration of 1 M in duplicates. Affinities of AVN-492 to both the 5-HT6R and 5-HT2BR were assessed in an equilibrium competitive [3H]LSD displacement assay. AVN-492 was provided at different concentrations and [3H]LSD was kept at a concentration of 1.50 nM for 5-HT6R, or 1.20 nM for 5-HT2BR. The ligands were added to corresponding receptor-membrane suspensions (plasma membranes obtained from engineered HeLa cells expressing recombinant human 5-HT6R or engineered CHO-K1 cells expressing recombinant human 5-HT2BR). The cell membrane/ligands mixtures were incubated in buffer of the following composition: For 5-HT6R: 50 mM Tris-HCl, pH 7.4, 150 mM NaCl, 2 mM ascorbic acid, 0.001% BSA – 120 min at 37?C; for 5-HT2BR: 50 mM Tris-HCl, pH 7.4, 4 mM CaCl2, 0.1% ascorbic acid – 60 min at 37?C. Specific radio-ligand binding was measured as a difference between total binding and binding in the presence of excessive concentration of cold serotonin [1].
动物实验	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) were used. Rodents were obtained from Jackson Laboratories and housed in a standard laboratory animal facility in groups of 5–7 animals per cage. Before entering the investigation, the animals were acclimated at least for seven days. Obese C57BL/6 male 18-week-old mice were obtained from Jackson Laboratories. The mice were fed on a high-fat diet (60% kcal Research Diet 12492i) from the age of 6 weeks. Upon arrival, the mice were maintained on the same high fat diet with free access to both food and water. The mice were individually housed in solid bottom static isolators with Bed-O'Cobs? bedding inside a BioBUBBLE? clean room that provided HEPA-filtered air into the clean room environment at a rate of 100 complete air changes per hour. All treatments and procedures including body weight determinations, drug administration, and glucose measurements were carried out in the clean room environment [1].

别名	AVN492
分子量	359.45
分子式	C17H21N5O2S
CAS No.	1220646-23-0

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 7.5 mg/mL (20.87 mM), Sonication is recommended.

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.782 mL	13.9101 mL	27.8203 mL	69.5507 mL
	5 mM	0.5564 mL	2.782 mL	5.5641 mL	13.9101 mL
	10 mM	0.2782 mL	1.391 mL	2.782 mL	6.9551 mL
	20 mM	0.1391 mL	0.6955 mL	1.391 mL	3.4775 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

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浓度 (终)

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参考文献

1. Ivachtchenko AV, et al. AVN-492, A Novel Highly Selective 5-HT6R Antagonist: Preclinical Evaluation. J Alzheimers Dis. 2017;58(4):1043-1063.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

AVN-492 1220646-23-0 GPCR/G Protein Neuroscience 5-HT Receptor inhibit Inhibitor Serotonin Receptor AVN492 AVN 492 5-hydroxytryptamine Receptor inhibitor

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AVN-492

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

相关产品

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剂量换算

体内实验配液计算器

技术支持

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