General description

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 µM 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.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Pelletier, J.C., et al. 2009. J. Med. Chem.52, 6962.

Packaging

Packaged under inert gas

10 mg in Glass bottle

Warning

Toxicity: Standard Handling (A)