nhe3 in 1

NHE3-IN-1 is a inhibitor of Na+/H+-exchanger 3 (NHE-3).

BI-9627 hydrochloride is a highly potent Na⁺/H⁺ exchanger 1 (NHE1) inhibitor. In intracellular pH recovery assays and human platelet swelling assays, its IC₅₀ values are 6 nM and 31 nM, respectively. It shows more than 30-fold selectivity over NHE2 and has no significant inhibitory effect on NHE3. BI-9627 hydrochloride can reduce the autophagy level of HTR-8/SVneo cells, significantly decrease the intracellular pH of human sperm, partially reverse the effect of DMA, and prolong the Ca²⁺ recovery time in KO hiPSC-CMs. BI-9627 hydrochloride has a low risk of drug-drug interactions, exhibits favorable pharmacokinetic properties in rats and dogs, and demonstrates potent activity in an ex vivo heart model of ischemia-reperfusion injury.

NHE3-IN-2 is an inhibitor of NHE3 (Na+/H+ exchanger-3), applicable for treating hypertension, thrombosis, and ischaemic diseases.

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