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.MedChemENecrostatin-1Cat. No.: HY-15760CAS No.: 4311-88-0Synonyms: Nec-1分式: CHNOS分量: 259.33作靶点: RIP kinase; Autophagy; Indoleamine 2,3-Dioxygenase (IDO)作通路: Apoptosis; Autophagy; Metabolic Enzyme/Protease储存式: Powder -20C 3 years4C 2 yea
2、rsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 46 mg/mL (177.38 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 3.8561 mL 19.2805 mL 38.5609 mL5 mM 0.7712 mL 3.8561 mL 7.7122 mL10 mM 0.3856 mL 1.9280 mL 3.8561 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
3、备液的保存式和期限。体内实验 Necrostatin-1 (Nec-1) is dissolved in DMSO (50 mg/mL) as stock. It is diluted in PBS before injection5.BIOLOGICAL ACTIVITY物活性 Necrostatin-1 (Nec-1)种有效,选择性和可渗透细胞的坏死性凋亡 (necroptosis) 抑制剂,在Jurkat细胞中的 EC50 为490 nM。Necrostatin-1 (Nec-1) 通过抑制坏死性凋亡途径中 (RIP1) 激酶域起作。1/3 Master of Small Molecul
4、es 您边的抑制剂师www.MedChemEIC50 & Target RIP1 kinase 1体外研究 Necrostatin-1 (Nec-1) is a specific and potent small-molecule inhibitor of cell death caused by death-domainreceptor (DR) stimulation in the presence of caspase inhibition in multiple cell types. Necrostatin-1 efficientlyinhibits the TNF-induced
5、necrotic death of L929 cells, which does not require exogenous caspase inhibitors1. Necrostatin-1 (Nec-1) prevents radiocontrast media (RCM)-induced dilation of peritubular capillaries,suggesting a novel role unrelated to cell death for the RIP1 kinase domain in the regulation of microvascularhemody
6、namics and pathophysiology of contrast-induced AKI (CIAKI) 2. The decreased viability of C6glioma cells caused by 3.0 M and 6.0 M shikonin is improved by pretreatment with Necrostatin-1 (Nec-1) to92.3% and 82.9% at 1.5 h and 84.4% and 78.6% at 3.0 h, respectively. Similarly, the viability of U87 gli
7、omacells is elevated by Necrostatin-1 to 91.6% and 81.5% at 1.5 h, and 81.8% and 71.2% at 3.0 h, respectively3. Necrostatin-1 (Nec-1) (30 M) increases the survival of cardiomyocyte progenitor cell (CMPCs) byinhibiting necrotic cell death 4.体内研究 Necrostatin-1 (Nec-1) induces tubular bilation and affe
8、cts the kinetics of the dilation of peritubular capillariesafter RCM application. Upon a single intraperitoneal application of a single dose of Necrostatin-1 (1.65 mg/kgbody weight, i.p.) 15 minutes before RCM, the return to baseline levels is prevented within the observationperiod 2.PROTOCOLCell As
9、say 3 C6 (3105 cells/well) and U87 (1.5105 cells/well) glioma cells are seeded onto 96-well microplate andcultured 24 h. PBS is added into the control group and Shikonin is added into experimental group to reachthe final concentration. Cellular viability is assessed using an MTT assay after Shikonin
10、 treatment atindicated time point. The absorbance value (A) at 570 nm is read using an automatic multi-wellspectrophotometer. Two groups of glioma cells from the same cell line are treated with Shikonin at lower orhigher concentration, respectively; other two groups of glioma cells are treated 1 h w
11、ith 100 M Necrostatin-1or 40 M z-VAD-fmk prior to co-incubation with Shikonin at indicated concentration. Additionally, another twogroups of glioma cells are treated only with 100 M Necrostatin-1 or 40 M Z-VAD-fmk at corresponding timepoint 3.MCE has not independently confirmed the accuracy of these
12、 methods. They are for reference only.Animal Mice 2Administration 8-10 week old male C57BL/6 mice (average weight approx.23 g) are used. Mice receive intravenousapplication of 200 L PBS or radiocontrast media (RCM) via the tail vein. A single dose of Z-VAD-fmk (10mg/kg body weight) or Necrostatin-1
13、(1.65 mg/kg body weight) is applied intraperitoneally 15 min. beforeRCM-injection. Mice are harvested another 24 hours after RCM-application (48 hours after reperfusion).Blood samples are obtained from retroorbital bleeding and serum levels of urea and creatinine aredetermined.MCE has not independen
14、tly confirmed the accuracy of these methods. They are for reference only.户使本产品发表的科研献2/3 Master of Small Molecules 您边的抑制剂师www.MedChemE Autophagy. 2019 Mar 20:1-12. ACS Appl Mater Interfaces. 2019 Apr 10;11(14):13123-13133. Cancer Lett. 2016 Aug 28;379(1):134-142. Cell Death and Disease (2019) 10:487
15、Cell Death Dis. 2019 Apr 15;10(5):331.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Degterev A, et al. Chemical inhibitor of nonapoptotic cell death with therapeutic potential for ischemic brain injury. Nat Chem Biol. 2005Jul;1(2):112-9.2. Linkermann A, et al. The RIP1-kinase
16、 inhibitor necrostatin-1 prevents osmotic nephrosis and contrast-induced AKI in mice. J Am SocNephrol. 2013 Oct;24(10):1545-57.3. Huang C, et al. Shikonin kills glioma cells through necroptosis mediated by RIP-1. PLoS One. 2013 Jun 28;8(6):e66326.4. Feyen D, et al. Increasing short-term cardiomyocyte progenitor cell (CMPC) survival by necrostatin-1 did not further preserve cardiacfunction. Cardiovasc Res. 2013 Jul 1;99(1):83-91.5. Zhou K, et al. RIP1-RIP3-DRP1 pathway regulates NLRP3 inflammasome activation following subar
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年医疗餐饮项目发展计划
- 2024年年环保装备合作协议书
- 2024年热压氮化硼制品项目建议书
- 【人教版】二年级数学下册导学案设计《重点单元知识归纳与易错总结 (3)》
- 2024年头孢菌素类药合作协议书
- 2024年有机磷系阻燃剂合作协议书
- 2024年办公商业空间设计合作协议书
- 一年级苏教版数学求未知数解析
- 苏教版四年级下册小学科学教学技巧
- 鲁迅笔下的人物
- 2024-2030年中国光电共封装(CPO)行业经营风险及可持续发展预测研究报告
- 合同审核流程及管理规定(2024年度)
- 2024年北京市劳动合同经典版(三篇)
- 重力与弹力 说课课件-2023-2024学年高一上学期物理人教版(2019)必修第一册
- 2024秋一年级道德与法治上册 第1课 开开心心上学去教案 新人教版
- 部编人教版四年级语文上册第1课《观潮》精美课件
- 《信息系统安全等级保护基本要求》
- Java网络编程技术01
- 2024国内各省市五星级酒店分布表全套
- 排球《正面上手发球》教案
- 外科医师晋升副高(正高)职称病例分析专题报告两篇
评论
0/150
提交评论