Na+/H+ Exchanger (NHE) Inhibitor

EIPA (L593754) is an orally active TRPP3 channel inhibitor with an IC₅₀ of 10.5 μM. EIPA also enhances autophagy by inhibiting Na⁺/H⁺-exchanger 3 (NHE3). EIPA inhibits macropinocytosis as well. EIPA can be used in the research of inflammation and cancers, such as gastric cancer, colon carcinoma, pancreatic carcinoma.

Cariporide (HOE-642) is a selective Na⁺/H⁺ exchange inhibitor.

Tenapanor (AZD1722) is a potent and orally active sodium/hydrogen exchanger isoform 3 (NHE3) inhibitor. Tenapanor reduces intestinal phosphate absorption predominantly through reduction of passive paracellular phosphate flux. Tenapanor has the potential for the research of hyperphosphatemia.

Zoniporide hydrochloride hydrate (CP-597396 hydrochloride hydrate) is a selective Na⁺/H⁺ exchanger subtype 1 (NHE1) inhibitor with cardioprotective activity, with IC₅₀ values of 67 nM and 73 nM against rat NHE1. Zoniporide hydrochloride hydrate reduces intracellular Na⁺ and Ca²⁺ overload, preserves mitochondrial integrity, activates pro-survival ERK1/2 and STAT3 signaling pathways, reduces necrosis and apoptosis, and decreases neutrophil aggregation. Zoniporide hydrochloride hydrate is applicable to research related to myocardial ischemia-reperfusion injury and heart graft ischemia-reperfusion injury.

Zoniporide (CP-597396) is a selective Na⁺/H⁺ exchanger subtype 1 (NHE1) inhibitor with cardioprotective activity, with IC₅₀ values of 67 nM and 73 nM against rat NHE1. Zoniporide reduces intracellular Na⁺ and Ca²⁺ overload, preserves mitochondrial integrity, activates pro-survival ERK1/2 and STAT3 signaling pathways, reduces necrosis and apoptosis, and decreases neutrophil aggregation. Zoniporide is applicable to research related to myocardial ischemia-reperfusion injury and heart graft ischemia-reperfusion injury.

Tenapanor (AZD1722) hydrochloride is a potent and orally active sodium/hydrogen exchanger isoform 3 (NHE3) inhibitor. Tenapanor hydrochloride reduces intestinal phosphate absorption predominantly through reduction of passive paracellular phosphate flux. Tenapanor hydrochloride has the potential for the research of hyperphosphatemia.

Rimeporide (EMD-87580) is a potent and selective inhibitor of the Na⁺/H⁺ exchanger (NHE-1).

BI-9627, a chemical probe, is a potent sodium-hydrogen exchanger isoform 1 (NHE1) inhibitor (IC₅₀ = 6 and 31 nM in intracellular pH recovery (pH_i) and human platelet swelling assays). BI-9627 displays >30-fold selectivity against NHE2 and with no measurable inhibitory activity against the NHE3 isoform. BI-9627 decreases autophagy in HTR-8/SVneo cells. BI-9627 can significantly reduce the pH_i of human sperm and partially reverse the effect of DMA. BI-9627 prolongs Ca²⁺ recovery time in KO hiPSC-CMs. BI-9627 shows low DDI (agent-agent interaction) potential, excellent pharmacokinetics in rat and dog, and remarkably potent activity in the isolated heart model of ischemia-reperfusion injury.

Dimethylamiloride is a specific antiporter inhibitor.

Eniporide hydrochloride (EMD-96785 hydrochloride) is a potent Na⁺/H⁺ exchange inhibitor.

S3226 is a highly selective NHE-3 inhibitor (IC₅₀<1 μM) that specifically blocks NHE-3-mediated sodium transport. S3226 significantly inhibits blastocyst formation and expansion in mouse embryos, and reduces fluid and electrolyte reabsorption in rat proximal tubules in a dose-dependent manner. S3226 effectively alleviates ischemia-induced acute renal failure by improving renal function parameters, reducing renal tubular injury and restoring intracellular pH homeostasis, without interfering with the normal tubuloglomerular feedback response. S3226 is widely used in studies of acute renal failure and related pathological mechanisms.

NHE3-IN-2 is a Na⁺/H⁺ exchanger-3 (NHE3) inhibitor ( patent WO2001079186A1, example 6-Chlor-4-phenyl-2-chinazolinyl-guanidin).

BI-9627 hydrochloride is a potent sodium-hydrogen exchanger isoform 1 (NHE1) inhibitor (IC₅₀ = 6 and 31 nM in intracellular pH recovery (pH_i) and human platelet swelling assays). BI-9627 hydrochloride displays >30-fold selectivity against NHE2 and with no measurable inhibitory activity against the NHE3 isoform. BI-9627 hydrochloride decreases autophagy in HTR-8/SVneo cells. BI-9627 hydrochloride can significantly reduce the pH_i of human sperm and partially reverse the effect of DMA. BI-9627 hydrochloride prolongs Ca²⁺ recovery time in KO hiPSC-CMs. BI-9627 hydrochloride shows low DDI (agent-agent interaction) potential, excellent pharmacokinetics in rat and dog, and remarkably potent activity in the isolated heart model of ischemia-reperfusion injury.

SGLT2-IN-2 (Compound E9) is an inhibitor of SGLT2. SGLT2-IN-2 significantly enhances the inhibition of SGLT2, NHE1, and SOD enzyme activity. SGLT2-IN-2 has protective effect on the glucose-free DMEM-induced injured cardiomyocytes. SGLT2-IN-2 significantly improves cardiac function in TAC-induced HF mice and inhibits cardiomyocyte hypertrophy as well as collagen deposition. SGLT2-IN-2 can ameliorate myocardial tissue damage and enhance mitochondrial autophagy in injured cardiomyocytes, thereby increasing survival rates in HF mice.

BMS-284640 is a synthetic sodium hydrogen exchange isomer-1 (NHE-1) inhibitor. BMS-284640 has a more than 380-fold higher NHE-1 inhibitory activity (IC50: 9 nM) compared to cariporide (HY-19693) and is more selective for NHE-1 over NHE-2 (IC50: 1.8 μM) and NHE-5 (IC50: 3.36 μM). BMS-284640 and its analogs also exhibit enhanced oral bioavailability and prolonged plasma half-life in rats..

RS5517 is a specific PDZ1-domain antagonist of NHERF1 that prevented its ectopic nuclear entry. RS5517 can be used for the research of colorectal cancer.

UTX-143 is an inhibitor of Na+/H+ exchange protein (NHE5). UTX-143 has antitumor activity.

NHE-1-IN-2 (compound 7g) is a potent NHE-1 inhibitor with an IC₅₀ of 0.78 μM. NHE-1-IN-2 alleviates left ventricular systolic dysfunction in mice model of heart failure.

Rimeporide (Standard) is the analytical standard of Rimeporide. This product is intended for research and analytical applications. Rimeporide (EMD-87580) is a potent and selective inhibitor of the Na+/H+ exchanger (NHE-1).

Zoniporide mesylate (CP-597396 mesylate) is a selective Na⁺/H⁺ exchanger subtype 1 (NHE1) inhibitor with cardioprotective activity, with IC₅₀ values of 67 nM and 73 nM against rat NHE1. Zoniporide mesylate reduces intracellular Na⁺ and Ca²⁺ overload, preserves mitochondrial integrity, activates pro-survival ERK1/2 and STAT3 signaling pathways, reduces necrosis and apoptosis, and decreases neutrophil aggregation. Zoniporide mesylate is applicable to research related to myocardial ischemia-reperfusion injury and heart graft ischemia-reperfusion injury.