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LP 922056 是一种具有口服活性的高效 Notum Pectinacetylesterase 抑制剂,在人和小鼠细胞试验中的 EC50 分别为 21 nM 和 55 nM。
Notum pectinacetylesterase inhibitor. Activates wnt signalling in vitro (EC50 values are 21 nM in human and 55 nM in mouse cell-based assay). Increases cortical bone thickness in mouse model of bone growth.
Tarver et al (2016) Stimulation of cortical bone formation with thienopyrimidine based inhibitors of Notum Pectinacetylesterase. Bioorg.Med.Chem.Lett 26 1525 PMID:26897593 |Brommage et al (2019) NOTUM inhibition increases endocortical bone formation and bone strength. Bone Res. 7 PMID:30622831
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