ZINC13407541 is a small molecule antagonist for FGF23, inhibits FGF-23 signaling with IC50 of 0.45 uM.
ZINC13407541 binds to FGF-23 and disrupts its interaction with the FGFR1/α-KL complex, inhibits FGF-23 activation of the FGFR/a-KL receptor complex.
ZINC13407541 caused significant -60 and 100% inhibition of FGF-23 stimulation of ERK reporter activity at 2.5 and 10 μM, respectively, in HEK293T cells, did not inhibit FGFR activation of these FGF ligands.
ZINC13407541 significantly increased serum phosphate, PTH, and 1,25(OH)2D, decreased serum abundance of FGF-23 by about 35% in Dmp1-null mice.
