下载本文档
版权说明:本文档由用户提供并上传,收益归属内容提供方,若内容存在侵权,请进行举报或认领
文档简介
1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEPhenylbiguanideCat. No.: HY-101331CAS No.: 102-02-3Synonyms: N-Phenylbiguanide; PBG; 1-Phenylbiguanide分式: CHN分量: 177.21作靶点: 5-HT Receptor作通路: GPCR/G Protein; Neuronal Signaling储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6
2、months-20C 1 month溶解性数据体外实验 DMSO : 150 mg/mL (846.45 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 5.6430 mL 28.2151 mL 56.4302 mL5 mM 1.1286 mL 5.6430 mL 11.2860 mL10 mM 0.5643 mL 2.8215 mL 5.6430 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,并请注意储备液的保存式和期限。体内实验请根据您的实验动物和给药式选择适当的溶解案,配制前请先
3、配制澄清的储备液,再依次添加助溶剂(为保证实验结果的可靠性,体内实验的作液,建议您现现配,当天使;澄清的储备液可以根据储存条件,适当保存;以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占):1. 请依序添加每种溶剂: 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (14.11 mM); Clear solution2. 请依序添加每种溶剂: 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (14.11 mM); Clear solution3.
4、请依序添加每种溶剂: 10% DMSO 90% corn oil1/3 Master of Small Molecules 您边的抑制剂师www.MedChemESolubility: 2.5 mg/mL (14.11 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Phenylbiguanide种选择性的 5-HT3 受体激动剂,EC50 为 3.00.1 M。IC50 & Target 5-HT3 Receptor3 M (EC50)体外研究 Phenylbiguanide (1-Phenylbiguanide) is a 5-HT3 receptor
5、selective agonist with pEC50s of 5.57, 4.07, and4.47 for r5-HT3A(b), h5-HT3A, m5-HT3A(b) , respectively 1. The effect of Phenylbiguanide (1-Phenylbiguanide hydrochloride) in promoting the growth of the HT29 cell line is investigated.Phenylbiguanide causes a dose dependent proliferation of HT29 cells
6、 after 48 hours incubation. Themaximum proliferation is at a 5HT concentration of 12.5 M (P0.01). Phenylbiguanide significantlystimulates the growth of cells at concentrations of 3.125 M (P0.05) and 6.25 M (P0.01) 2.体内研究 In anaesthetised mice, Phenylbiguanide (PBG), a drug that is known to stimulate
7、 cardiopulmonary afferent C-fibres,is injected into the right atrium of the heart and mapped c-Fos expression within specific regions of thecentral nervous system. Intraatrial injection of PBG produces a reflex cardiorespiratory response including apronounced bradycardia and a respiratory depression
8、 3.PROTOCOLCell Assay 2 HT29 cells are washed with Phosphate buffer saline (PBS) and harvested with a 0.5% trypsin solution at 50-60% confluency. Cells are then added to wells at a density of 104 cells/well in a 96-well plate to a finalvolume of 100 L/well. After 24 hours of incubation at 37C in a 5
9、% CO2 atmosphere, the culture medium isreplaced with 200 L fresh culture medium containing 5HT hydrochloride, Phenylbiguanide hydrochloride atconcentrations of: 3.125, 6.25, 12.5, 25, 50, and 100 M . Cells cultured solely in media served as negativecontrols. After 48 hours of incubation at 37C in a
10、5% CO2 atmosphere, the culture medium is removed and8 L MTT reagent (diluted in PBS at a concentration of 4 mg/mL) is added to 50 L of fresh culture mediumat a final concentration of 0.55 mg/mL. The optimum incubation period time is determined in a pilot study 2.MCE has not independently confirmed t
11、he accuracy of these methods. They are for reference only.Animal Mice 3Administration 3 Adult male specified pathogen free (SPF) BALB/c mice (28-33 g; n=10) are used throughout this study. Allmice have free access to water and food in a light (12: 12 h light/ dark cycle, lights on at 0700 h) andtemp
12、erature-controlled (21-23C) environment. Mice are randomly assigned to two treatment groups, 1) intra-atrial injection of 0.9% saline (controls, n=5) or 2) intra-atrial injection of vehicle containing Phenylbiguanide(n=5). For the PBGinjected group, mice are injected with an effective dose of Phenyl
13、biguanide (1-1.5 g in10-15 L saline) . This is repeated five times in total with each injection separated by 8-10 min. For controlmice, each mouse receives five saline injections (10-15 L each), also at 8-10 min intervals 3.MCE has not independently confirmed the accuracy of these methods. They are
14、for reference only.2/3 Master of Small Molecules 您边的抑制剂师www.MedChemEREFERENCES1. Mair ID, et al. Pharmacological characterization of a rat 5-hydroxytryptamine type3 receptor subunit (r5-HT3A(b) expressed in Xenopuslaevis oocytes. Br J Pharmacol. 1998 Aug;124(8):1667-74.2. Ataee R, et al. Study of 5H
15、T3 and HT4 receptor expression in HT29 cell line and human colon adenocarcinoma tissues. Arch Iran Med.2010 Mar;13(2):120-5.3. de Vries A, et al. Characterisation of c-Fos expression in the central nervous system of mice following right atrialinjections of the 5-HT3receptor agonist Phenylbiguanide. Auton Neurosci. 20
温馨提示
- 1. 本站所有资源如无特殊说明,都需要本地电脑安装OFFICE2007和PDF阅读器。图纸软件为CAD,CAXA,PROE,UG,SolidWorks等.压缩文件请下载最新的WinRAR软件解压。
- 2. 本站的文档不包含任何第三方提供的附件图纸等,如果需要附件,请联系上传者。文件的所有权益归上传用户所有。
- 3. 本站RAR压缩包中若带图纸,网页内容里面会有图纸预览,若没有图纸预览就没有图纸。
- 4. 未经权益所有人同意不得将文件中的内容挪作商业或盈利用途。
- 5. 人人文库网仅提供信息存储空间,仅对用户上传内容的表现方式做保护处理,对用户上传分享的文档内容本身不做任何修改或编辑,并不能对任何下载内容负责。
- 6. 下载文件中如有侵权或不适当内容,请与我们联系,我们立即纠正。
- 7. 本站不保证下载资源的准确性、安全性和完整性, 同时也不承担用户因使用这些下载资源对自己和他人造成任何形式的伤害或损失。
最新文档
- 2024至2030年风冷式空气预冷机项目投资价值分析报告
- 2024至2030年茶巾消毒柜项目投资价值分析报告
- 2024至2030年深层卸妆棉项目投资价值分析报告
- 2024至2030年中国双绉绣花夜衣行业投资前景及策略咨询研究报告
- 2024至2030年丝杠保护套项目投资价值分析报告
- 2024年鸡翅木满雕十八汉地屏项目可行性研究报告
- 2024年透明质酸壳聚糖项目可行性研究报告
- 医药产业园区规划与运营管理
- 2024年中国荔枝蓉市场调查研究报告
- 2024年中国网层图书架市场调查研究报告
- 2024年执业药师继续教育专业答案
- 非ST段抬高型急性冠脉综合征诊断和治疗指南(2024)解读
- 口腔诊所传染病预防措施
- 国家开放大学电大《计算机应用基础(本)》学士学位论文家用电器销售管理系统的设计与实现
- 刑事诉讼法学(湘潭大学)智慧树知到期末考试答案2024年
- 教师语言与沟通艺术智慧树知到期末考试答案2024年
- 北京市西城区2023-2024学年五年级上学期期末数学试卷
- 部编版五年级上册语文第八单元作文课-推荐一本书教学课件
- 纯电动车冷却性能计算按流量[共2页]
- 三国群英传4全秘籍
- 报价单(模板)
评论
0/150
提交评论