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Merck
CN
  • Experimental solubility profiling of marketed CNS drugs, exploring solubility limit of CNS discovery candidate.

Experimental solubility profiling of marketed CNS drugs, exploring solubility limit of CNS discovery candidate.

Bioorganic & medicinal chemistry letters (2010-11-09)
Yun W Alelyunas, James R Empfield, Dennis McCarthy, Russell C Spreen, Khanh Bui, Luciana Pelosi-Kilby, Cindy Shen
摘要

We determined the experimental solubility of CNS marketed drugs. Of the 98 drugs measured, greater than 90% had solubility >10 μM in pH 7.4 buffer. Only seven drugs had solubility <10 μM. Using these data, we established a solubility criterion to support CNS discovery. The implication of poor solubility with potential safety concerns and undesirable side effects are discussed.

材料
Product Number
品牌
产品描述

Sigma-Aldrich
布洛芬, ≥98% (GC)
Supelco
布洛芬
Sigma-Aldrich
加巴喷丁, solid
Sigma-Aldrich
5,5-二苯基海因, ≥98%
Sigma-Aldrich
(±)-止呕灵
Sigma-Aldrich
2-丙基戊酸
Sigma-Aldrich
利鲁唑, solid
Sigma-Aldrich
布洛芬, meets USP testing specifications
Sigma-Aldrich
(±)-Vigabatrin
Sigma-Aldrich
卡马西平, meets USP testing specifications