NHE3-IN-3 (Compound 1) is a potent inhibitor of the isoform 3 of the Na+ H+ exchanger (NHE3). It exhibits pIC50 values of 6.2 and 6.6 against human and rat NHE3, respectively. Furthermore, NHE3-IN-3 showcases exceptional oral bioavailability of 98% in Sprague–Dawley rats [1].