Sciex 6500+ QTrap Mass Spectrometer

Sciex 6500 QTrap 质谱仪

• 批准号: 10177437
• 负责人: Michael Darin Cameron
• 金额: $ 48.58万
• 依托单位: SCRIPPS FLORIDA
• 依托单位国家: 美国
• 财政年份: 2021
• 资助国家: 美国
• 起止时间: 2021-06-15 至 2022-06-14
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/10177437
• 关键词: Contract Services; Data; Dose; Drug Industry; Drug Kinetics; Evaluation; Florida; Funding; Grant; Institution; Investments; Laboratories; Life; Maintenance; Manufacturer Name; Mus; Plasma; Research Project Grants; Running; Sampling; System; Techniques; Testing; Tissue Sample; United States National Institutes of Health; base; cost; design; drug metabolism; experience; instrument; mass spectrometer; pre-clinical; repaired; sample collection; small molecule

Project Summary/Abstract This proposal seeks funds to purchase a Sciex 6500+ Qtrap mass spectrometer with integrated Sciex M5 microflow UHPLC to become part of the drug metabolism and pharmacokinetic (DMPK) core. This system will be used to quantitate the concentration of small molecules in plasma and tissue samples from mouse pharmacokinetic studies. The Sciex 6500 Qtrap is ideally suited to this function and is the workhorse instrument for the analysis of PK samples in pre-clinical laboratories in the pharmaceutical industry. The Scripps DMPK core runs over 200 mouse PK studies per year and, when possible, utilizes microsampling techniques. Microsampling requires superior analytical sensitivity because the technique collects a limited sample, 5-10 µl plasma. The advantage of microsampling is that it allows triplicate PK data to be generated from three mice, instead of using twelve or twenty-four mice as have traditionally been required. Analysis of mouse pharmacokinetic samples in the Scripps DMPK core is currently done on a Sciex 5500 mass spectrometer. Microsampling techniques are currently utilized for approximately 80% of the compounds tested at the Scripps DMPK core. The decision to use microsampling or revert to a traditional large sample collection design using higher numbers of mice is based on the planned dose and an evaluation of the analytical limit of quantitation, which is determined prior to conduct of the in-life portion of the PK study. This shared instruments currently supports a range of research projects originating from multiple NIH funded projects associated with seven institutions. The level of engagement for each of these projects with the DMPK core is high, and the core is written into multiple HIN funded grants. To maximize the impact of NIHs investment and assure the instrument remains productive for a period of at least five years, Scripps guarantees maintenance and operational costs, including staff to oversee the instrument, and will purchase a service contract with the instrument manufacturer that will cover all repairs and yearly preventative maintenance for five years. This shared instrument will be installed in the Scripps Florida DMPK core and will be operated by a group of experienced mass spectroscopists within the DMPK core.

项目总结/摘要 该提案寻求资金购买Sciex 6500+ Qtrap质谱仪， 集成Sciex M5微流UHPLC，成为药物代谢的一部分， 药代动力学（DMPK）核心。该系统将用于定量小分子的浓度， 来自小鼠药代动力学研究的血浆和组织样品中的分子。Sciex 6500 Qtrap非常适合此功能，是PK分析的主力仪器 制药行业临床前实验室的样品。Scripps DMPK核心运行 每年进行200多项小鼠PK研究，并在可能的情况下利用微量取样技术。 微量取样需要上级分析灵敏度，因为该技术收集有限的 样品，5-10 µl血浆。微量采样的优点是，它允许一式三份PK数据， 由三只老鼠产生，而不是像传统上那样使用十二只或二十四只老鼠。 必需的.目前已完成Scripps DMPK核心中小鼠药代动力学样本的分析 Sciex 5500质谱仪上微取样技术目前用于 在斯克里普斯DMPK核心测试的化合物中，约有80%的化合物。决定使用 微采样或恢复到传统的大样本收集设计，使用更高数量的 基于计划剂量和定量分析限的评价， 在进行PK研究的活体部分之前确定。这种共享工具 目前支持一系列来自NIH资助项目的研究项目 与七家机构合作。这些项目中的每一个项目与 DMPK核心很高，核心被写入多个HIN资助的赠款。最大化 国家卫生研究院投资的影响，并确保该工具在至少一段时间内保持生产力 五年，斯克里普斯保证维护和运营成本，包括工作人员监督 仪器，并将与仪器制造商购买服务合同， 五年内的所有维修和年度预防性维护。这一共同文书将是 安装在斯克里普斯佛罗里达DMPK核心，并将由一组经验丰富的质量 DMPK核心的光谱分析师

项目成果

1,3-Diphenylureido hydroxamate as a promising scaffold for generation of potent antimalarial histone deacetylase inhibitors.

• DOI: 10.1038/s41598-023-47959-z
• 发表时间: 2023-11-29
• 期刊: Scientific reports
• 影响因子: 4.6

Structure-Activity Relationship and Biological Investigation of a REV-ERBα-Selective Agonist SR-29065 (34) for Autoimmune Disorders.

REV-ERBα-选择性激动剂 SR-29065 (34) 治疗自身免疫性疾病的结构-活性关系和生物学研究。

• DOI: 10.1021/acs.jmedchem.3c01413
• 发表时间: 2023
• 期刊: Journal of medicinal chemistry
• 影响因子: 7.3
• 作者: He,Yuanjun;Zhu,Di;Greenman,Kevin;Ruiz,Claudia;Shang,Jinsai;Lu,Qun;Kojetin,DouglasJ;Drakas,Robert;Cameron,MichaelD;Lizarzaburu,Mike;Solt,LauraA;Kamenecka,TheodoreM
• 通讯作者: Kamenecka,TheodoreM