TRPM5 inhibitor NDNA is potent and selecive TRPM5 inhibitor, inhibits Ca2+- induced TRPM5 currents with IC50 of 2.4 nM.
NDNA binds to a region critical for channel gating, stabilizes the ion-conducting pore in an apo-like closed conformation.
NDNA inhibits Ca2+-induced TRPM5 activation in a non-competitive manner.
NDNA enhances insulin release, GLP-1 release, and insulin sensitivity.
TPPO dose-dependently inhibited acidic pHe-induced MMP-9 production in B16-BL6 cells (IC50=41 uM), but did not reduce cell viability.
NDNA (10 mg/kg. s.c.) significantly reduced spontaneous lung metastasis, without affecting tumor growth, body weight, or CBG, in tumor bearing mice.
