Chemiluminescent nitrogen detection (CLND) to measure kinetic aqueous solubility.
Chemiluminescent nitrogen detection (CLND) to measure kinetic aqueous solubility.
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DOI：
10.1002/9780470559277.ch130145
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发表时间：
2013-01-01
影响因子：
--
通讯作者：
Placko, Steven
中科院分区：
文献类型：
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作者：
Kestranek, Aimee;Chervenak, Andrew;Placko, Steven
溶解度是体外研究的剂量限制性质，因此是药物发现中测量的关键理化性质。溶解度数据可用于指导铅的优化，排除不稳定的生物测定结果，并确定潜在的下游责任，如生物测定或口服生物利用度不足的溶解度。通常，早期的体外研究使用制备为二甲基亚砜（DMSO）储备溶液的库化合物进行，得到含有低浓度DMSO的体外测试溶液（
Solubility is the dose-limiting property for in vitro studies, and therefore is a critical physicochemical property to measure in drug discovery. Solubility data can be used to guide lead optimization, troubleshoot erratic bioassay results, and identify potential downstream liabilities such as insufficient solubility for bioassays or oral bioavailability. Typically, early in vitro studies are performed using library compounds prepared as dimethylsulfoxide (DMSO) stock solutions, resulting in in vitro test solutions containing DMSO at low concentration (