PROTAC/分子胶药物研发服务
PROTAC分子DMPK评价常见问题与解决方案:
时间:2022-08-22
来源:澳门永利welcome
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【摘要】:
DMPK Issue Recommendation
Solubility Insoluable Simulated fluid replace PBS buffer
Permeability Poor recovery Addition of BSA,FBS
Transporter Substrate, or inhibitor Specific transporter, hMDR1 Knockin MDCKll Cells Or, hBCRP Knockin MDCKll Cells
Bioanalysis Unstable Deactivate enzyme in plasma or blood immediately
Bioanalysis Non specific binding Detergent
Bioanalysis Fragment inLs-MS ion source Optimized MS condition
Metabolism Diverse metabolism Comprehensive metabolism system: microsome, hepatocyte, S9,cytosol;AO,UGT activity;  CYP phenotyping
PPB Unstable Enzyme inhibitor
In vivo PK Low bioavailability No fasting
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