Na+/K+ ATPase Inhibitor

3-Methylcrotonylglycine-d₂ is the deuterated-labeled 3-Methylcrotonylglycine (HY-113232). 3-Methylcrotonylglycine is an organic acid conjugate associated with leucine catabolism that inhibits respiratory chain complex II-III, mitochondrial creatine kinase, and synaptic membrane Na⁺, K⁺-ATPase. 3-Methylcrotonylglycine increases reactive oxygen species levels to mediate oxidative damage, while inhibiting mitochondrial electron transport, reducing tricarboxylic acid cycle flux, and interfering with intracellular energy transport and neuronal ion homeostasis. 3-Methylcrotonylglycine is a neurotoxic metabolite that accumulates in the metabolic pathway of 3-methylcrotonyl-CoA carboxylase deficiency. 3-Methylcrotonylglycine can be used in studies related to 3-methylcrotonyl-CoA carboxylase deficiency.

Chamigrenol is a Na⁺/K⁺-ATPase inhibitor with an IC₅₀ value of 15.9 μg/mL. Chamigrenol shows strong inhibitory activities against Gram-positive and Gram-negative bacteria except Escherichia coli, with MIC values of 50 µg/mL.

(-)-γ-Cuparenol is a sesquiterpene compound with an IC₅₀ of 23.6 μg/mL against porcine Na⁺/K⁺-ATPase. (-)-γ-Cuparenol reduces phytohemagglutinin (PHA)-induced activation of NF-AT and NF-κB in Jurkat cells. (-)-γ-Cuparenol inhibits the growth of Gram-positive bacteria and some Gram-negative bacteria. (-)-γ-Cuparenol exhibits weak inhibitory activity against Candida albicans. (-)-γ-Cuparenol is applicable for research related to immunoregulation, cardiovascular diseases and bacterial infections.

3-Methylglutaric acid (Standard) is the analytical standard of 3-Methylglutaric acid (HY-113410). This product is intended for research and analytical applications. 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.

Lithospermoside (Griffonin) (Standard) is the analytical standard of Lithospermoside (HY-N0821). This product is intended for research and analytical applications. Lithospermoside is an orally active Na⁺/K⁺-ATPase inhibitor and hypoglycemic agent. Lithospermoside increases intracellular sodium levels in normal and sickle red blood cells. Lithospermoside reduces fasting blood glucose levels, improves glucose tolerance, and prevents weight loss in diabetic mice. Lithospermoside can be used in the research of sickle cell disease and diabetes.

Omeprazole-d₃-1 is the deuterium labeled Omeprazole. Omeprazole-1 (H 16868) is an orally active H⁺,K⁺-ATPase inhibitor and a proton pump inhibitor. Omeprazole-1 competitively inhibits CYP2C19, CYP3A4, and CYP2C9 activity. Omeprazole-1 inhibits gastric acid secretion and can be used for acid-related gastrointestinal disorders. Omeprazole-1 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-1 alters small intestinal morphology and magnesium absorption, and induces gastric mucosa morphologic changes. Omeprazole-1 also has neuroprotective and antibacterial effects.

16-HETE is arachidonic acid metabolite through subterminal hydroxylation by cytochrome P-450. 16-HETE exhibits vasodilatory and PMN inhibitory effects and serves as biomarker for early stages of non-alcoholic fatty liver disease.

Chloroprocaine (2-Chloroprocaine) is a potent inhibitor of Na,K-ATPase activity with an IC₅₀ of 13 mM. Chloroprocaine blocks peripheral nerve.

V-161 is the orally active inhibitor for Na⁺-V-ATPase with an IC₅₀ of 144 nM. V-161 inhibits Enterococcus hirae and Vancomycin-resistant Enterococcus faecium (VRE) under alkaline condition with MIC of 4 µg/mL and 4 µg/mL. V-161 inhibits colonization of VRE in mouse small intestine.

AU-461 is an orally active and reversible inhibitor of the gastric H⁺/K⁺ ATPase with IC₅₀ values for rabbit-derived and pig-derived enzymes are 12.15 μM and 4.20 μM respectively. AU-461 competes with activated cationic K⁺ (Kᵢ = 1.64 μM). AU-461 reduces both histamine-stimulated gastric acid secretion and basal gastric acid secretion in rats. AU-461 inhibits ulcer formation caused by ethanol or sodium hydroxide, and restores the plasma gastrin level to normal. AU-461 can be used for the study of peptic ulcers.

Prilocaine (hydrochloride) (Standard) is the analytical standard of Prilocaine (hydrochloride). This product is intended for research and analytical applications. Prilocaine hydrochloride, an amino amide, is a Na/K-ATPase inhibitor. Prilocaine has neurotoxic effects.

Hsp90-IN-38 (compound 20m) is a HSP90 (heat shock protein) inhibitor. Hsp90-IN-38 exhibits strong HSP90 binding affinity with a K_d of 87 nM. Hsp90-IN-38 inhibits ATPase with an IC₅₀ of 0.13 μM. Hsp90-IN-38 inhibits HCT116, MCF-7, SKBr3, K562 and A549 cells with IC₅₀s of 0.187, 0.072, 0.105, 0.403 and 031 μM, respectively.

Tegoprazan (CJ-12420; RQ-00000004), a potassium-competitive acid blocker, is a reversible, oral active and highly selective inhibitor of gastric H+/K+-ATPase that could control gastric acid secretion and motility, with IC₅₀ values ranging from 0.29-0.52 μM for porcine, canine, and human H⁺/K⁺-ATPases in vitro. Tegoprazan significantly improves colitis in mice and enhances the intestinal epithelial barrier function. Tegoprazan is promising for research of Inflammatory bowel, gastric acid-related, motilityimpaired diseases.

Gitoxin (Standard) is the analytical standard of Gitoxin (HY-136933). This product is intended for research and analytical applications. Gitoxin is a degradation metabolite of Digitoxin (HY-B1357) and a non-competitive Na⁺/K⁺-ATPase inhibitor, with an IC₅₀ of 1.18e-6 M against the porcine high-affinity subtype and an IC₅₀ of 2.85e-5 M against the porcine low-affinity subtype. Gitoxin regulates atrial contractility and rhythmicity. Gitoxin is applicable to research related to congestive heart failure.

AR-HO47108 is an orally active reversible Na+/K+ ATPase inhibitor. AR-HO47108 reversibly blocks the final step of gastric acid secretion by competitively binding to the potassium ion binding site of the Na+/K+ ATPase in the gastric wall cells. AR-HO47108 can be used for research on diseases related to excessive gastric acid secretion, such as peptic ulcers.

ME-3407 (EF-4040) is a H⁺-K⁺-ATPase redistribution disruptor and myosin light chain kinase (MLCK) and protein kinase A inhibitor. ME-3407 blocks gastric acid secretion and aminopyrine accumulation by inhibiting microsomal-to-apical membrane redistribution of H⁺-K⁺-ATPase and suppressing MLCK-mediated myosin light chain phosphorylation. ME-3407 is promising for research of peptic ulcer.

Leminoprazole (NC 1300O3) is an inhibitor for acid pump, H⁺ K⁺-ATPase,. Leminoprazole stimulates the secretion and synthesis of gastric mucus, attenuates gastric ulcers. Leminoprazole is orally active.

SPAI-1 is a specific inhibitor for monovalent cation transporting ATPases. SPAI-1 is a peptide isolated from porcine duodenum, inhibits Na⁺, K⁺-ATPase and H⁺, K⁺-ATPase in vitro, stimulates Mg²⁺-ATPase.

PROTAC PI3K/110β degrader-2 is a VHL-recruiting PI3K/110β PROTAC degrader, with DC₅₀ values of 1.258 μM and 2.185 μM in MCF-7/ADM and A549/DDP cells, respectively. PROTAC PI3K/110β degrader-2 induces proteasomal degradation of PI3K/110β, inhibits phosphorylation of AKT and expression of Bcl-2, while suppressing the activity and expression of P-gp. It also induces endoplasmic reticulum stress and mitochondrial apoptosis via the PERK/CHOP pathway. PROTAC PI3K/110β degrader-2 exerts anti-tumor activity against multidrug-resistant cancer cells both in vitro and in vivo, and produces a synergistic effect when combined with Doxorubicin (HY-15142A) or Cisplatin (HY-17394), making it applicable for the research of multidrug-resistant cancers.

ASI-222 is an aminosugar cardiac glycoside. ASI-222 can inhibit Na+/K+ ATPase and show positive inotropic effect. ASI-222 can be used for the research of cardiovascular disease.