sodium/hydrogen exchanger

Monensin sodium salt (Monensin A sodium salt) is an antibiotic secreted by Streptomyces cinnamaticus and acts as an ion carrier that mediates Na+/H+ exchange. Monensin is an effective inhibitor of Wnt signaling. Monensin causes a significant increase in multivesicular bodies (MVBs) and regulates exosome secretion. Monensin sodium salt exhibits biological activities including anticoccidial, antibacterial, antitumor, and cell signaling regulatory effects. Monensin sodium salt can be used in studies of cellular ion transport and metabolism.

Cariporide (HOE-642) (HOE-642), an effective NHE1 inhibitor, has inhibitory effects on the degranulation of human platelets, the formation of platelet-leukocyte-aggregates, and the activation of the GPIIb/IIIa receptor (PAC-1).

Rimeporide (EMD-87580) (EMD-87580) is a potent and selective Sodium hydrogen exchange 1 (NHE-1) inhibitor.

Rimeporide hydrochloride (EMD-87580 hydrochloride) is a potent and selective inhibitor of Sodium hydrogen exchange 1 (NHE-1).

Tenapanor (RDX 5791) is an inhibitor of the sodium-proton (Na(+)/H(+)) exchanger NHE3, which plays a prominent role in sodium handling in the gastrointestinal tract and kidney. Tenapanor possesses an excellent preclinical safety profile and, as of now, there are no serious concerns about its side effects.

EIPA (L593754) is a TRPP3 channel inhibitor (IC50=10.5 μM) and an inhibitor of Na+/H+ exchange (NHE). EIPA inhibits megacytosis, promotes autophagy, and can be used in inflammation and tumor studies.

BI-9627 is a selective and potent sodium hydrogen exchange isomer 1 (NHE1) inhibitor.BI-9627 partially reverses the effects of DMA with IC50 values of 6 and 31 nM in the intracellular pH recovery (pHi) and human platelet lysis assays.BI-9627 is often used as a negative control for BI-0054, which can be used for the study of ischemia-reperfusion injury in isolated hearts. BI-9627 is often used as a negative control for BI-0054 and can be used to study ischemia-reperfusion injury in isolated hearts.

KR-32568 is a sodium/hydrogen exchanger 1 (NHE-1) inhibitor (IC50: 230 nM) with potent cardioprotective effects. At a concentration of 10 μM, it restored cardiac systolic function in an isolated ischemic rat heart model. Additionally, KR-32568 (0.3 mg/kg) reduced myocardial infarction size in a rat model of ischemia and reperfusion injury.

Zoniporide hydrochloride hydrate is a potent and selective sodium-hydrogen exchanger type 1 (NHE-1) inhibitor. Zoniporide hydrochloride hydrate inhibits human NHE-1 with IC50 of 14 nM.

Repunapanor (compound 123) is a potent inhibitor of the sodium/hydrogen exchanger isoform 3 [Na+/H+ exchanger 3 (NHE-3)].

Sodium-hydrogen exchanger isoform 1 (NHE1) inhibitor

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.

2-Oxo-zoniporide hydrochloride is an orally active type 1 sodium-hydrogen exchanger (NHE-1) inhibitor, utilized in the study of myocardial ischemic injuries.