生物试剂
>
生化试剂
>
信号通路
> YM348
加入收藏 取消收藏

YM348  

促销价¥{{model.attbuying.price}}

市场价¥0.00

累计销量0 累计评价0 人评论

别称 {{model.alias}}
中文名称 {{model.name}}
英文名称 {{model.enname}}
品牌 {{model.brand}}
CAS {{model.cas}}
分子式
分子量 {{model.molecularweight}}
MDL {{model.mdl}}
货号 {{model.procode}}
数量

+ -

件 库存{{model.attbuying.number}}件
立即购买 加入购物车 下载说明书

看了又看
包装规格：5mg in glass bottle
产品描述：基本信息 产品编号： V10108 产品名称： YM348 CAS: 372163-84-3   储存条件 粉末 -20℃ 四年     分子式： C14H17N3O 溶于液体     分子量 243.30     化学名：  YM-348; 2-(7-Ethyl-1H-furo[2,3-g]indazol-1-yl)-1(S)-methylethylamine Solubility (25°C)：   体外:   DMSO   Ethanol   Water   体内(现配现用):   ＜1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 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。   生物活性 产品描述 一种口服有效的 5-HT2C 受体激动剂，对克隆的人类 5-HT2C 受体具有高亲和力，Ki 为 0.89nM。 靶点 HT2A Receptor 13nM (Ki) 5-HT2B Receptor 2.5nM (Ki) 5-HT2C Receptor 0.89nM (Ki) HT2A Receptor 93nM (EC50) HT2B Receptor 3.2nM (EC50) HT2C Receptor 1nM (EC50) 体外研究 YM348 has high affinity for cloned human 5-HT2C receptors with a Ki value of 0.89nM and lower affinities for human-cloned 5-HT2B (Ki : 2.5nM) and 5-HT2A receptors (Ki : 13nM). To assess the binding specificity of YM348, a broad evaluation of an additional 46 binding sites including several other 5-HT receptor subtypes (1A, 1B, 1D, 3, 4, 5A, 6, 7) is performed. IC50 values of YM348 are found to be >1μM for all of the binding sites except for the human 5-HT1A receptors (Ki : 130nM), bovine 5-HT1D receptors (Ki : 481nM), human 5-HT7 receptors (Ki : 177nM), and human α2A receptors (Ki : 126nM).YM348 exhibits a fullagonistic activity on human 5-HT2A and 5-HT2B receptors. The EC50 values of YM348 for 5-HT2C, 5-HT2A, and 5-HT2B receptors are 1.0, 93 and 3.2nM, respectively . 体内研究 Oral administration of YM348 induces penile erections and hypolocomotion in rats, being completely inhibited by a selective 5-HT2C receptor antagonist, SB242084. YM348 inhibits spontaneous activity in a dose-dependent manner with a minimum effective dose of 0.203 mg/kg .   推荐实验方法(仅供参考) Kinase Assay Experiments are performed with membranes obtained from Chinese Hamster Ovary (CHO) cells expressing human 5-HT2C or 5-HT2A receptors and Human Embryonic Kidney 293-Epstein-Barr virus nuclear antigen (HEK293-EBNA) cells expressing human 5-HT2B receptors. Binding assays with [3H] 5-HT are carried out. The reaction medium (50mM Tris-HCl buffer (pH 7.4) containing 4 mM CaCl2, 10 M pargyline and 0.1 mg/ml L-(+)-ascorbic acid) containing [3H] 5-HT, membrane preparation and test compounds are incubated at 37°C for 30 min. Nonspecific binding is determined in the presence of 10 M 5-HT, and specific binding is calculated as the total binding minus the nonspecific binding. After incubation, 4mL of 50mM Tris-HCl buffer (pH 7.4) containing 4mM CaCl2 is added, and the medium is filtrated under decompression through a Whatman GF/Bglass filter pretreated with 0.1% polyethyleneimine. The filter is washed with the same buffer solution (4mL×3). The glass filter is immersed in 6 mL of liquid scintillator (Packard, Aquasol-2), and the radioactivity is measured with a liquid scintillation counter. The amount of protein is measured. The dissociation constants (Kd values) are obtained by Scatchard analysis using SAS (ver. 6.11). The concentrations of compounds showing 50% inhibition of receptor binding, IC50 values, are obtained by nonlinear analysis using SAS (ver. 6.11). The Ki values indicating affinity for receptors are calculated   Animal Administration Rats Male Wistar rats (215-350 g) are used. Rats are administered YM348 (0.0677, 0.203, 0.677, and 2.03 mg/kg) orally and moved again to their home cages. After 20 min, thereafter, the rats are individually placed in transparent acrylic plastic cages (35×30×18 cm), and their motor activity is measured for 40 min. The measurements are carried out using a SUPER-MEX sensor. SB242084 (0.1-3 mg/kg i.p.) is administered 30 min before YM348 treatment.
保存条件：-20℃

猜你喜欢