Na+/K+ ATPase Inhibitor

Bifenazate is a carbazate acaricide that control 100% of mites at a concentration of 25 ppm. Bifenazate is a positive allosteric modulator of GABA receptor. Bifenazate is the inhibitor for the mitochondrial electron transport chain complex III.

Chlorpropamide is an oral hypoglycemic agent that can influence acetaldehyde metabolism in mice and has a potentiating effect on antidiuretic hormone.

Transdermal Peptide Disulfide TFA (TD 1 Disulfide(peptide) TFA) is a 11-amino acid peptide, binds to Na⁺/K⁺-ATPase beta-subunit (ATP1B1), and mainly interacts with the C-terminus of ATP1B1. Transdermal Peptide Disulfide TFA can enhance the transdermal delivery of many macromolecules.

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.

Lithospermoside (Griffonin) 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.

Bafilomycin C1 is a macrolide antibiotic isolated from Streptomyces sp. Bafilomycin C1 is a potent, specific and reversible inhibitor of vacuolar-type H⁺-ATPases (V-ATPases). Bafilomycin C1 inhibits growth of gram-positive bacteria and fungi. Bafilomycin C1 induces cell apoptosis and can be used for the study of hepatocellular carcinoma (HCC).

Omeprazole (Standard) is the analytical standard of Omeprazole. This product is intended for research and analytical applications. 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.

Omeprazole-d₃ (H 16868-d₃) is deuterium labeled Omeprazole. 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.

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.

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.

(+)-SJ733 is an anti-malaria agent which can also inhibit Na⁺-ATPase PfATP4.

Omeprazole-¹³C,d₃ is a ¹³C-labeled and deuterium labeled Omeprazole. 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.

12(R)-HETE is a CYP-dependent arachidonic acid metabolite that acts as a proinflammatory lipid mediator. 12 (R)-HETE widely exists in various tissues including the eye, skin and liver. In the cornea, 12(R)-HETE is metabolized via pathways such as β-oxidation into the precursor of 12(R)-HETrE. Without direct receptor binding, 12(R)-HETE indirectly activates AHR-mediated target gene transcription, while inhibiting the enzymatic activity of Na+,K+-ATPase and the intracellular calcium elevation induced by TP agonists. 12(R)-HETE also possesses multiple physiological effects such as chemotaxis, proangiogenesis, vasodilation, natriuresis, diuresis and intraocular pressure reduction, and can be widely used in studies related to psoriasis, inflammatory skin diseases and ocular inflammation.

Brazilein is a compound with anti-inflammatory and neuroprotective activities, with an IC₅₀ of 500 μM against guinea pig Na⁺,K⁺-ATPase. Brazilein reduces iNOS mRNA expression, thereby inhibiting nitric oxide production in immune cells. Brazilein suppresses inflammatory responses by reducing the mRNA expression of TNF-α and IL-6, but has no effect on IL-1β expression. Brazilein reduces the cerebral infarction volume and improves the neurological function scores of rats with cerebral ischemia-reperfusion injury. Brazilein induces apoptosis of splenic lymphocytes in mice. Brazilein inhibits humoral immune responses in mice, and causes thymus and spleen atrophy as well as body weight loss in mice. Brazilein also possesses antimalarial and antibacterial activities. Brazilein is also a red dye. Brazilein can be used in studies related to the infection, nervous system, cardiovascular system and inflammatory diseases.

7,8-Dimethoxycoumarin is a coumarin compound derived from Artemisia caruifolia with oral activity. 7,8-Dimethoxycoumarin inhibits mitochondrial permeability transition pore and H⁺/K⁺-ATPase, and exhibits antioxidant, anti-inflammatory, renoprotective, neuroprotective and gastroprotective effects. 7,8-Dimethoxycoumarin reduces lipid peroxidation (TBARS), increases GSH levels, inhibits myeloperoxidase (MPO) activity, and regulates the expression of inflammatory factors by inhibiting the NF‑κB and MAPK pathways. 7,8-Dimethoxycoumarin ameliorates gastric mucosal injury, alleviates renal tissue lesions and relieves neuropathic pain. 7,8-Dimethoxycoumarin can be used in studies related to acute renal failure, trigeminal neuralgia and gastritis.

17-HETE is arachidonic acid metabolite through cytochrome P-450 pathways, which consists of 17R-HETE and 17S-HETE enantiomers. 17-HETE serves as allosteric activator of the cytochrome P450 1B1 and inhibitor of ATPase, induces cardic hypertrophy.

Marinobufogenin is a strong inhibitor of Na⁺/K⁺ ATPase that has been identified in mammalian plasma.

Antcin A is an orally active modulator of p53 and glucocorticoid receptor (GR), with an IC₅₀ of 8.55 μM against human GR. Through transcriptional activation of p53, Antcin A induces miR-200c and inhibits ZEB1, regulates epithelial-mesenchymal transition markers, and suppresses cancer cell migration/invasion. Antcin A activates GR, inhibits Na⁺/K⁺-ATPase and NLRP3 inflammasome assembly, pyroptosis (pyroptosis) and pro-inflammatory cytokine release, reduces hepatic lipid deposition, improves liver function, and reverses metabolic changes induced by the SARS-CoV-2 spike protein. Antcin A can be used in research related to breast cancer, head and neck cancer, non-alcoholic fatty liver disease, and coronavirus disease 2019 (COVID-19).

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

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