Table 1.

Inhibition of select transporters in cell-based assays by test compounds

TargetTenapanor pIC50NTX792 pIC50NTX3572 pIC50
Human NHE3, prompt8.3±0.38.6±0.28.0
Rat NHE3, prompt8.0±0.38.4±0.48.9±0.1
Rat NHE3, persistent8.4±0.38.16.2±0.1
Human NaPi2b≤5.0n.a.n.a.
Human PiT1≤5.0n.a.n.a.
  • Inhibition response curves for compounds in each assay are expressed as pIC50. Results from several determinations are expressed as means±SDs. pIC50, negative log of the concentration that inhibits response by 50%; n.a., not measured.