Na+/K+ ATPase Inhibitor

Omeprazole (H 16868) is an orally active H⁺,K⁺-ATPase inhibitor and a proton pump inhibitor. Omeprazole competitively inhibits CYP2C19, CYP3A4, and CYP2C9 activity. Omeprazole inhibits gastric acid secretion and can be used for acid-related gastrointestinal disorders. Omeprazole inhibits pancreatic cancer cell proliferation, induces apoptosis, autophagosome accumulation (elevated LC3-I and LC3-II levels), oxidative stress, and cytogenetic imbalance, modulates lysosomal transport, reduces inflammatory cytokines. Omeprazole alters small intestinal morphology and magnesium absorption, and induces gastric mucosa morphologic changes. Omeprazole aslo has neuroprotective and antibacterial effects.

Ginsenoside Rb1, a main constituent of the root of Panax ginseng, inhibits Na⁺, K⁺-ATPase activity with an IC₅₀ of 6.3±1.0 μM. Ginsenoside also inhibits IRAK-1 activation and phosphorylation of NF-κB p65 .

Bufalin is an active component isolated from Chan Su, acts as a potent Na⁺/K⁺-ATPase inhibitor, binds to the subunit α1, α2 and α3, with K_d of 42.5, 45 and 40 nM, respectively. Anti-cancer activity.

ATPase-IN-7 (Example 1) is a H⁺/K⁺-ATPase inhibitor. ATPase-IN-7 is used in the research of gastrointestinal inflammatory diseases and gastric acid-related diseases.

Cassaine (Nervocidine) is a Na⁺/K⁺-ATPase inhibitor. Cassaine stabilizes phosphorylated intermediates, slows spontaneous dephosphorylation and blocks potassium-stimulated dephosphorylation. Cassaine exhibits non-competitive inhibition with respect to K⁺, shows inhibition enhanced by Pi and antagonized by Na⁺. Cassaine induces positive inotropic effects in perfused hearts with faster inotropy offset. Cassaine can be used for research on cardiac arrhythmias.

Tolbutamide is an orally active K_ATP inhibitor. Tolbutamide inhibits cell proliferation, stimulates exocytosis of glucagon and reduces fetal lethality of mice. Tolbutamide can be used in the research of diabete.

Istaroxime hydrochloride is a Na⁺/K⁺-ATPase inhibitor (IC₅₀=0.11 μM) and a sarcoplasmic/endoplasmic reticulum calcium ATPase 2 (SERCA 2) activator.

Deslanoside (Desacetyllanatoside C) is a rapidly acting cardiac glycoside used to treat congestive heart failure and supraventricular arrhythmias due to reentry mechanisms, and to control ventricular rate in the treatment of chronic atrial fibrillation. Deslanoside inhibits the Na-K-ATPase membrane pump, resulting in an increase in intracellular sodium and calcium concentrations .

Omeprazole (H 16868) sodium is an orally active H⁺,K⁺-ATPase inhibitor and a proton pump inhibitor. Omeprazole sodium competitively inhibits CYP2C19, CYP3A4, and CYP2C9 activity. Omeprazole sodium inhibits gastric acid secretion and can be used for acid-related gastrointestinal disorders. Omeprazole sodium inhibits pancreatic cancer cell proliferation, induces apoptosis, autophagosome accumulation (elevated LC3-I and LC3-II levels), oxidative stress, and cytogenetic imbalance, modulates lysosomal transport, reduces inflammatory cytokines. Omeprazole sodium alters small intestinal morphology and magnesium absorption, and induces gastric mucosa morphologic changes. Omeprazole sodium aslo has neuroprotective and antibacterial effects.

Gramicidin S (Gramicidin soviet) is a cationic cyclic peptide antibiotic that selectively targets bacterial cell membranes and has anticancer activity. Gramicidin S also exerts antibacterial activity by destroying membrane integrity and interfering with membrane protein function. Gramicidin S inserts into the phospholipid bilayer through hydrophobic amino acid residues, specifically binds to negatively charged membrane lipids and disrupts membrane structure, thereby inhibiting cell division and cell wall synthesis, and ultimately causing bacterial death. Gramicidin S also inhibits ion channels, with IC₅₀s of 41 μM, 24 μM, and 3 μM for Na⁺/K⁺-ATPase, tobacco leaf plasma membrane Mg²⁺/K⁺-ATPase, and rat heart plasma membrane Ca²⁺-ATPase, respectively.

Biacetyl monoxime (Diacetyl monoxime), a myosin ATPase inhibitor, is a skeletal and cardiac muscle contraction inhibitor. Biacetyl monoxime is also a well-characterized non-competitive inhibitor of chemical and motile activity of skeletal muscle myosin-II. Biacetyl monoxime induces sarcoplasmic reticulum Ca²⁺ release.

Acevaltrate inhibits the Na⁺/K⁺-ATPase activity in the rat kidney and brain hemispheres with IC₅₀s of 22.8 μM and 42.3 μM, respectively.

Strophanthidin is a naturally available cardiac glycoside. Strophanthidin 0.1 and 1 nmol/L increases and 1~100 μmol/L inhibits the Na+/K+-ATPase activities, but Strophanthidin 10 and 100 nmol/L does not affect Na+/K+-ATPase activities in cardiac sarcolemmal. Strophanthidin increases both diastolic and systolic intracellular Ca²⁺ concentration.

Magnesium Lithospermate B, is a derivative of caffeic acid tetramer and an inhibitor of Na+/K+ ATPase, which can be extracted from Salviae miltiorrhizae. Magnesium Lithospermate B is widely used for the research of cardiovascular diseases, and it can protect against glucose-induced intracellular oxidative damage. Magnesium Lithospermate B also suppresses neuroin?ammation and attenuates neurodegeneration.

Tolbutamide (Standard) is the analytical standard of Tolbutamide. This product is intended for research and analytical applications. Tolbutamide is an orally active K_ATP inhibitor. Tolbutamide inhibits cell proliferation, stimulates exocytosis of glucagon and reduces fetal lethality of mice. Tolbutamide can be used in the research of diabete.

Oleandrin (PBI-05204) inhibits the Na⁺, K⁺-ATPase activity with an IC₅₀ of 620 nM.

Telocinobufagin (Telobufotoxin; Telocinobufogenin) is an orally active bufadienolide with potential anti-tumor effects. Telocinobufagin exerts its anti-cancer effects on non-small cell carcinoma, osteosarcoma, thyroid cancer, breast cancer and head and neck squamous cell carcinoma by inhibiting the STAT3, JAK2/STAT3, LARP1-mTOR, PI3K/Akt/Snail and PLK1 pathways, and can also induce tumor cell apoptosis. Telocinobufagin enhances the Th1 immune response and protects against Salmonella typhimurium infection. Telocinobufagin has a strong cardiac-stimulating effect by inhibiting the activity of Na⁺/K⁺-ATPase, and it can promote renal fibrosis. Telocinobufagin demonstrates non-opioid analgesic effects in various acute pain models.

3-Methylglutaric acid is a non-selective inhibitor of mitochondrial function and Na⁺, K⁺-ATPase, with an inhibition rate of 30% on rat cortical synaptosomal Na⁺, K⁺-ATPase. 3-Methylglutaric acid can induce reactive oxygen species (ROS) generation, thereby causing oxidative damage and inhibiting mitochondrial redox potential and ion pump function of cell membranes. 3-Methylglutaric acid can be used to study the neuropathological mechanisms of metabolic diseases and the role of oxidative stress-mediated neuronal damage in neurodegeneration.

Tegoprazan (CJ-12420), a potassium-competitive acid blocker, is a reversible, orally active and highly selective inhibitor of gastric H⁺/K⁺-ATPase. Tegoprazan inhibits gastric acid secretion and motility against porcine, canine and human H⁺/K⁺-ATPase with IC₅₀ values ranging from 0.29-0.52 μM in vitro. Tegoprazan significantly improves colitis and enhances the intestinal epithelial barrier function in mice. Tegoprazan is promising for research of Inflammatory bowel, gastric acid-related, motilityimpaired diseases.

Neriifolin, a CNS-penetrating cardiac glycoside, is an inhibitor of the Na⁺, K⁺-ATPase. Neriifolin can target beclin 1, inhibits the formation of LC3-associated phagosomes and ameliorates experimental autoimmune encephalomyelitis (EAE) development. Neriifolin induces cell cycle arrest and apoptosis in human hepatocellular carcinoma HepG2 cells^[2.