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Beschreibung

A 2-aminopyrimidine compound that counteracts the antagonizing effect of Dkk-1 (Dickkopf-1) against Wnt-3a/LRP5 interaction and prevents Dkk-1-mediated Kr2/LRP5/Dkk-1 complex formation and internalization. Shown to successfully rescue cellular response to Wnt-3a stimulation in the presence of Dkk-1 (EC50 = 0.63 µ,M in a cell-based TCF-luciferase assay) in vitro and double the tibia trabecular bone formation in OVX rats in a period of 28 days via an oral dose of 10 mg/kg/day in vivo.