化合物 AVN-492|T5179|TargetMol

价格	￥297	￥745	￥1230
包装	1mg	5mg	10mg

最小起订量	1mg
发货地	上海
更新日期	2025-11-17

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产品详情

中文名称:化合物 AVN-492	英文名称:AVN-492
CAS:1220646-23-0	品牌: TargetMol
产地: 美国	保存条件: Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
产品类别: 抑制剂
货号: T5179

Product Introduction

Bioactivity

名称	AVN-492
描述	AVN-49 is a potent and selective 5-HT6R Antagonist (Ki: 91 pM).
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].
体外活性	AVN-492与[3H]LSD竞争结合到5-HT6R的亲和力估计为91 pM（IC50^b = 194 pM）。相比之下，AVN-492对5-HT2BR的亲和力，Ki^b = 170 nM（IC50^b = 268 nM）。尽管AVN-492会被人类微粒体代谢，但在高达10 M浓度下，它并没有显著抑制五种主要的人类重组CYP同工酶，即CYP3A4、1A2、2C9、2C19和2D6 [1]。
体内活性	AVN-492在啮齿动物中具有高口服生物利用度和良好的脑渗透性。在行为测试中，AVN-492在提高加迷宫模型中表现出抗焦虑效应，防止了阿波吗啡引起的惊跳起始脉冲抑制（PPI模型）的破坏，并逆转了东莨菪碱和MK-801引起的被动避免模型中的记忆缺损。在小鼠模型中未发现AVN-492具有抗肥胖效应[1]。
存储条件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
溶解度	DMSO : 7.5 mg/mL (20.87 mM), Sonication is recommended. 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 1 mg/mL (2.78 mM), Sonication is recommended.
关键字	Serotonin Receptor \| Inhibitor \| inhibit \| AVN-492 \| AVN 492 \| 5-hydroxytryptamine Receptor \| 5HTReceptor \| 5-HT6 \| 5-HT Receptor \| 5HT Receptor
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关键字： AVN492|TargetMol

公司简介

TargetMol Chemicals Inc. 总部位于马萨诸塞州波士顿，致力于为全球生化领域科学家的研究提供专业的产品和服务。TargetMol?品牌的客户群分布于40多个国家和地区，已发展成为全球知名的化合物库和小分子化合物研究供应商。 TargetMol?可提供160多种满足不同需求的化合物库，以及多种类型的生化试剂产品，包括12000多种抑制剂、16000多种天然产物和各类多肽、抗体、生命科学试剂盒等，此外，我们还建设有CADD（计算机辅助药物设计）研究中心、药理实验室、药化合成平台三大技术中心，全方位满足客户的定制需求。凭借我们优质的产品和服务、快速高效的全球供应链和专业的技术支持，我们将有效帮助您缩短研发周期，取得更成功的结果。

成立日期	2013-04-18 （13年）	注册资本	566.265100万人民币
员工人数	100-500人	年营业额	￥ 1亿以上
主营行业	天然产物,生化试剂,分子生物学,分子砌块,生物技术服务	经营模式	贸易,工厂,试剂,定制,服务

TargetMol中国（陶术生物）

VIP 4年

公司成立：13年
注册资本：566.265100万人民币
企业类型：有限责任公司(自然人投资或控股)
主营产品：小分子抑制剂、药物筛选化合物库、药物筛选等
公司地址：静安区江场三路238号8楼

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