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.MedChemEDHEACat. No.: HY-14650CAS No.: 53-43-0Synonyms: Prasterone; Dehydroisoandrosterone;Dehydroepiandrosterone分式: CHO分量: 288.42作靶点: Androgen Receptor; Endogenous Metabolite作通路: Others; Metabolic Enzyme/Protease储存式: Powder -20C 3 year
2、s4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 50 mg/mL (173.36 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 3.4672 mL 17.3358 mL 34.6717 mL5 mM 0.6934 mL 3.4672 mL 6.9343 mL10 mM 0.3467 mL 1.7336 mL 3.4672 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
3、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 (8.67 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 (8.
4、67 mM); Clear solution1/3 Master of Small Molecules 您边的抑制剂师www.MedChemE3. 请依序添加每种溶剂: 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (8.67 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 DHEA (Prasterone)最丰富的类 醇激素之。 DHEA通过多种信号传导途径介导其作,并通过转化成雄激素和雌激素衍物(例如,雄激素,雌激素,7和7 DHEA (Prasterone),以及7和7表雄甾酮衍物)通过其特异性受体起作。IC50
5、 & Target Human Endogenous Metabolite体外研究 DHEA (Prasterone) is an effective antiapoptotic factor, reversing the serum deprivation-induced apoptosis inprostate cancer cells (DU145 and LNCaP cell lines) as well as in colon cancer cells (Caco2 cell line). DHEA(Prasterone) significantly reduces serum de
6、privation-induced apoptosis in all 3 cancer cell types, quantitatedwith the APOPercentage assay (apoptosis is reduced from 0.5870.053 to 0.1420.0016 or 0.0590.002after treatment for 12 hours with DHEA or NGF, respectively; n=3, P50: 11.23.6 nM and 12.42.2 nM inDU145 and Caco2 cells, respectively) 1.
7、 DHEA (Prasterone) is the principal sex steroid precursor inhumans and can be converted directly to androgens. DHEA (Prasterone) (1 M) causes a dose-dependentinhibition of Chub-S7 proliferation, as assessed by thymidine incorporation assays. DHEA (Prasterone)treatment inhibits expression of the key
8、glucocorticoid-regulating genes H6PDH (100 nM) and HSD11B1 (1M) in differentiating preadipocytes in a dose-dependent manner. In keeping with this finding, DHEA(Prasterone) treatment (1 M) results in a marked reduction in 11-HSD1 oxoreductase activity (1 M) anda concurrent increase in dehydrogenase a
9、ctivity at the highest DHEA dose used (25 M DHEA) indifferentiated adipocytes 2.体内研究 DHEA (Prasterone) in the diet (0.45 % w/w) of male B6 mice (groups of five mice) treated for 8 weeks led tosignificant decreases in body temperature compared with mice fed the control AIN-76A diet. A similarcomparis
10、on indicated that control and pair-fed mice are also significantly different. Animals fed DHEA(Prasterone) have significantly lower temperatures than mice fed the control diet 26/29 times tested; micepair fed to those on the DHEA (Prasterone) diet are less affected, with 8/29 values significantly lo
11、wer than inmice fed AIN-76A ad libitum. The temperatures of mice fed DHEA (Prasterone) or pair fed to DHEA(Prasterone) are significantly different 21/29 times tested. Body weights are significantly greater in mice fedthe control diet than in mice fed DHEA or pair fed to DHEA (Prasterone). Food intak
12、e (grams per day) fromcages are averaged for each week (n=7), except for Week 9 (n=3). The amount of food intake is significantlydecreased in mice fed DHEA (Prasterone). By design, mice pair fed to DHEA (Prasterone) ate about thesame amount. Thus, it appears that DHEA (Prasterone) reduces body tempe
13、rature by food restriction and bya separate mechanism 3.PROTOCOLCell Assay 2 Chub-S7 preadipocytes and human primary preadipocytes are seeded into a 24-well plate at densities 1105and 2.5105 respectively. Following overnight culture, medium is supplemented with DHEA, androstenediol,2/3 Master of Sma
14、ll Molecules 您边的抑制剂师www.MedChemEor DHEA (Prasterone) (0-100 M). Following 24-, 48-, or 72 h incubation, cell proliferation is assessed byincubation with radiolabeled thymidine (0.2 Ci/well) for the final 6 h of culture. Proteins are precipitated withTCA, and cells are scraped in NaOH. The respective
15、 content of radiolabeled nuclear material in the resultinglysates is analyzed by scintillation counting 2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Mice 3Administration 3 Mice are fed Purina Lab Chow until the start of experiments (Day 0).
16、Groups of five mice are then fedpelleted AIN-76A diet containing either no additive or DHEA (0.45% w/w) between 0900 and 1000 hr. Dietsare stored at 4C for no longer than six months to maintain optimal activity. Mice are given the diets adlibitum, except for mice that are pair fed to mice treated wi
17、th DHEA (Prasterone). The amounts of AIN-76Adiet the pair-fed mice received are determined by the weight of food consumed by the DHEA-fed mice on adaily basis. Body weights (grams) are measured at different time points starting at Day 1 and ending at Day59. Daily food intakes (grams per day) are det
18、ermined by weighing the food consumed per cage of five mice.The meanSEM values are calculated for weeks 1 to 8 (n=7); week 9 had only 3 days.MCE has not independently confirmed the accuracy of these methods. They are for reference only.户使本产品发表的科研献 Toxicol Appl Pharmacol. 2019 Jun 5:114612.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Anagnostopoulou V, et al. Differential effects of dehydroepiandrosterone and testosterone in prostate and colon cancer cell apoptosis:the role of nerve grow
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
- 成本实操-养生馆成本核算案例
- 2026年吉林省汪清县中考物理押题试卷含解析
- 安徽省砀山县2026届中考联考物理试题含解析
- 山东省潍坊市青州市益都中学2026届中考四模物理试题含解析
- 中医儿科护理的食疗方法
- 山西省阳泉市平定县重点中学2026年中考试题猜想物理试卷含解析
- 中医护理产科护理课件
- 中医眼保健护理工作坊
- 巴音郭楞蒙古自治州和静县2025届数学四年级下学期期中学业水平测试模拟试题(含解析)
- 中职护理护理职业培训教材课件
- 电梯日常安全管理和作业人员职责培训
- 2026湖南省材料谷科技发展有限公司招聘5人笔试参考试题及答案解析
- 2026湖南省中考英语作文预测六大主题12篇范文
- 系统动力学视角下建筑工程项目风险管理的深度剖析与实践探索
- 2026春人教版六年级语文下册期末综合复习提纲(完整版)
- 2026年辽宁高考物理题库含答案
- 2026年威海预售房合同(1篇)
- 2025年有权单独巡视高压设备人员考试试卷及答案
- 2026年十堰市中小学教师职称晋升水平能力测试题及答案
- 2026人教版小学三年级语文下册期末考试卷及答案
- 门诊护理流程优化及患者满意度提升
评论
0/150
提交评论