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.MedChemEPyributicarbCat. No.: HY-111202CAS No.: 88678-67-5Synonyms: TSH-888分式: CHNOS分量: 330.44作靶点: Cytochrome P450作通路: Metabolic Enzyme/Protease储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 100 m
2、g/mL (302.63 mM; Need ultrasonic)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (7.57 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 (7.57 mM); Suspended solution; Need ultrasonic1/2 Master of Small Molecules 您边的抑制剂师www.MedChemE3. 请依序添加每种溶剂: 1
3、0% DMSO 90% corn oilSolubility: 2.5 mg/mL (7.57 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Pyributicarb种氨 甲酸酯型除草剂, CYP3A4 因和类孕烷 X 受体 (hPXR) 的有效激活剂。IC50 & Target CYP3A4 1, hPXR 2体外研究 Pyributicarb, a carbamate-type herbicide, is a potent activator of both CYP3A4 gene and human pregnane Xreceptor (hPXR)
4、. Pyributicarb is found to increase the CYP3A4 reporter activity at 0.1 to 1 M more stronglythan typical CYP3A4 inducer rifampicin. Expression of hPXR-siRNA clearly diminishes the Pyributicarb-stimulated CYP3A4 reporter activity in 3-1-10 cells and decreases the endogenous CYP3A4 mRNA levels inHepG2
5、 cells 1. Pyributicarb induces luciferase transcription via hPXR at low concentrations in the order of10 nM. The relative potency of Pyributicarb for hPXR is 8.6-fold that of rifampicin (RIF) 2.体内研究 Pyributicarb causes enhancement of CYP3A4-derived reporter activity in mouse livers introduced with h
6、PXRby adenovirus 1.PROTOCOLCell Assay 1 HepG2-derived cells stably expressing the CYP3A4 reporter gene (3-1-10 cells) are used in this experiment.The cells are treated with 0.3 to 30 M Pyributicarb for 48 h. Then reporter activities are determined 1.MCE has not independently confirmed the accuracy o
7、f these methods. They are for reference only.Animal Male ICR mice (5 weeks old) are used and fed standard rodent chow. After 18-h fasting, mice are injected i.v.Administration 1 with adenovirus 4.0 109 50% titer culture infectious dose (TCID50)/mouse. Three days after the infection,vehicle (0.5% met
8、hyl cellulose/saline) or Pyributicarb (100 mg/kg/day) is administered p.o. for 2 consecutivedays. Animals are killed 20 h after the last dose 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Matsubara T, et al. Assessment of human pregnane
9、 X receptor involvement in pesticide-mediated activation of CYP3A4 gene. DrugMetab Dispos. 2007 May;35(5):728-33.2. Kojima H, et al. Comparative study of human and mouse pregnane X receptor agonistic activity in 200 pesticides using in vitro reportergene assays. Toxicology. 2011 Feb 27;280(3):77-87.McePdfHeightCaution: Product has not been fully validated for medic
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
- 水力机械结构课程设计
- 装修质量保证合同(范本)
- 自建房商铺租赁合同(范本)
- 水泥制品模具设计与制造考核试卷
- unit6(基础作业)2024-2025学年六年级上册 英语 译林版
- 汽轮机运行人员技能提升与培训考核试卷
- D打印技术在空间探索领域的应用考核试卷
- 办公文具消费者行为与市场趋势考核试卷
- 草原割草对草原生物多样性的长期影响考核试卷
- 软件项目冲突管理考核试卷
- 小学数学课题《小学生良好的数学学习习惯的培养策略》开题报告
- 译林版九年级上学期英语第一次月考试卷(含答案解析)
- 橡胶行业定义与分类报告
- 饲料厂车间岗位质量操作规范
- GB/T 43462-2023电化学储能黑启动技术导则
- 2024年九省联考广西新高考政治试卷(含答案)
- 麻醉药品管理培训课件
- 幼儿园公开课:中班语言《跑跑镇》有声动态课件
- 以瞄准我的妹妹没剪板
- 垃圾能源回收
- 钛及钛合金阳极氧化膜 编制说明
评论
0/150
提交评论