na+/k+ atpase

8-[(2,6-dimethylbenzyl)amino]-2,3-dimethylimidazo[1,2-a]pyridine-6-car is a H+/K+ ATPase inhibitor with IC50 of 0.38μM.

Sodium oleate (cis-9-Octadecenoic acid sodium salt) (Oleic acid sodium) is an abundant monounsaturated fatty acid sodium. Sodium oleate is a Na+/K+ ATPase activator.

Transdermal Peptide acetate(888486-23-5 free base) (TD 1 (peptide) acetate) is a 11-amino acid peptide, binds toNa+/K+-ATPase beta-subunit (ATP1B1), and mainly interacts with the C-terminus of ATP1B1. Transdermal Peptide can enhance the transdermal delivery of many macromolecules.Transdermal Peptide TD 1 Amide is novel peptide designed to enhance transdermal drug delivery.

Rostafuroxin (PST 2238) has been used in trials studying the treatment of Essential Hypertension.

Oleic acid (Glycon Wo) is a natural product, a common monounsaturated fatty acid found in a variety of animal and vegetable fats and oils. Palmitic acid is a Na+/K+ ATPase activator.

Cinobufagin (Cinobufagine) is a selective Na+/K+-ATPase inhibitor. The activity of Cinobufagin is same as ouabain.

Phlorizin (Phloridzin) is a non-selective SGLT inhibitor found in apple, for hSGLT1( Ki=300 nM) and hSGLT2( Ki=39 nM) .

Bufalin is an active ingredient and one of the glycosides in the traditional Chinese medicine ChanSu; it is also a bufadienolide toxin originally isolated from the venom of the Chinese toad Bufo gargarizans, with potential cardiotonic and antineoplastic a

Suloctidil is a peripheral vasodilator that was formerly used in the management of peripheral and cerebral vascular disorders. It is hepatotoxic and fatalities have occurred.

1. Oleandrin (Folinerin), the principal cardiac glycoside component of PBI-524, can quantitatively account for regulation of BDNF at both the protein and transcriptional levels. 2. Oleandrin are known to inhibit the Na, K-ATPase pump, resulting in a consequent increase in calcium influx in heart muscle. 3. Oleandrin has stronger anti-proliferative activity in undifferentiated CaCO-2 cells (IC50, 8.25 nM) , causes an autophagic cell death and altered ERK phosphorylation in undifferentiated.

14-Anhydrodigitoxigenin is a cardenolide and a derivative of digitoxin.1 It reduces the activity of guinea pig heart Na+/K+-ATPase by 15% when used at a concentration of 10 μM.2

Caloxin 2A1 TFA is a peptide inhibitor specifically targeting the extracellular plasma membrane Ca2+-ATPase (PMCA), without influencing the basal activities of Mg2+-ATPase or Na+-K+-ATPase[1].

Transdermal Peptide is a 11-amino acid peptide, binds to Na+/K+-ATPase beta-subunit (ATP1B1), and enhances the transdermal delivery of many macromolecules. Transdermal Peptide (TD1) binds to ATP1B1, and mainly interacts with the C-terminus of ATP1B1 in yeast and mammalian cells. The interaction affects the expression and localization of ATP1B1 and epidermal structure, but can be antagonized by the exogenous competitor ATP1B1 or be inhibited by ouabain. Inhibition of Transdermal Peptide binding to ATP1B1 causes decreased delivery of macromolecular drugs across the skin[1]. [1]. Wang C, et al. Role of the Na(+)/K(+)-ATPase beta-subunit in peptide-mediated transdermal drug delivery. Mol Pharm. 2015 Apr 6;12(4):1259-67.

Prilocaine hydrochloride (Prilocaine HCl) is a local anesthetic of the amino amide type, binds to voltage-gated sodium ion channels in the neuronal membrane, thereby preventing the permeability of sodium ions.

Digoxigenin monodigitoxoside is a cardiac glycoside metabolite of digoxin and a Na+/K+ ATPase inhibitor.

Stauntosaponin A and stauntosaponin B show moderate inhibitory activities against Na+/K+-ATPase with IC50 values of 21 and 29 uM, respectively.

Chlorpropamide (Diabinese) is a sulfonylurea hypoglycemic agent used in the treatment of non-insulin-dependent diabetes mellitus not responding to dietary modification.

Aquastatin A is a fungal metabolite originally isolated fromF. aquaeductuumthat has diverse biological activities.1It is active againstS. aureus(MIC = 32 μg/ml) and inhibits enoyl-acyl carrier protein reductase (Fabl; IC50= 3.2 μM) andS. aureusfatty acid synthesis (IC50= 3.5 μM).2Aquastatin A also inhibits the Na+/K+-ATPase and H+/K+-ATPase (IC50s = 7.1 and 6.2 μM, respectively), as well as protein tyrosine phosphatase 1B (PTP1B; IC50= 0.19 μM).1,3 1.Hamano, K., Kinoshita-Okami, M., Minagawa, K., et al.Aquastatin A, an inhibitor of mammalian adenosine triphosphatases from Fusarium aquaeductuum. Taxonomy, fermentation, isolation, structure determination and biological propertiesJ. Antibiot. (Tokyo)46(11)1648-1657(1993) 2.Kwon, Y.-J., Fang, Y., Xu, G.-H., et al.Aquastatin A, a new inhibitor of enoyl-acyl carrier protein reductase from Sporothrix sp. FN611Biol. Pharm. Bull.32(12)2061-2064(2009) 3.Seo, C., Soh, J.H., Oh, H., et al.Isolation of the protein tyrosine phosphatase 1B inhibitory metabolite from the marine-derived fungus Cosmospora sp. SF-5060Bioorg. Med. Chem. Lett.19(21)6095-6097(2009)

Citreoviridin, a toxin from Penicillium citreoviride NRRL 2579, inhibits brain synaptosomal Na+/K+-ATPase whereas, in microsomes, both Na+/K+-ATPase and Mg2+-ATPase activities are significantly stimulated in a dose-dependent manner.

Bassianin, a fungal metabolite identified in Beauveria, demonstrates inhibition of Mg2+-, Ca2+-, and Na+/K+-ATPase activities in equine erythrocyte ghosts, with inhibition rates of 81%, 58%, and 23%, respectively, at a concentration of 200 µg/ml. Additionally, bassianin exhibits cytotoxic properties against Sf9 and Sf21 insect cells, with 50% cytotoxic concentration (CC50) values of 4.91 µM and 12.12 µM, respectively.

(R)-Tegoprazan, a benzimidazole derivative, serves as a potent inhibitor of kidney H+/K+-ATPase, demonstrating significant efficacy with an IC50 of 98 nM against canine kidney Na+/K+-ATPase. This compound shows promise for research in gastrointestinal diseases.

Prilocaine acetate, an amino amide compound, functions as a Na/K-ATPase inhibitor, exhibiting neurotoxic effects [1] [2].

Istaroxime is an effective inhibitor of Na+, K+-ATPase (IC50: 0.11 μM).

Tenellin is a fungal metabolite that inhibits Mg2+-, Ca2+-, and Na+/K+-ATPase activities in erythrocytes. Tenellin is cytotoxic to Sf9 and Sf21 insect cells.

2,3-Butanedione 2-Monoxime (Diacetyl monoxime) is an inhibitor of skeletal and cardiac muscle contraction.

Strophanthidin (Strophanthidine) can induce calcium overload in vivo.

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

Carsatrin succinate is the salt form of Carsatin, a purinylpiperazine derivative used as a cardiotonic and antiarrhythmic. Carsatrin acts as positive inotropic agent that increases twitch tension and prolongs the action potential (AP) duration of ventricular muscle without affecting the Na+, K+-ATPase, adenylyl cyclase, phosphodiesterase isozymes, or cardiac myofilaments. Carsatrin’s positive inotropic effect can be prevented by tetrodotoxin but not by the adrenergic antagonists timolol, yohimbine, or prazosin.

11-Dehydrocorticosterone is an endogenous mineralocorticoid. It increases Na+/K+-ATPase mRNA expression in vascular smooth muscle cells and inhibits aldosterone action in B. marinus toad bladder tissue in a concentration-dependent manner. 11-Dehydrocorticosterone decreases the sodium/creatine ratio and increases the potassium/creatine ratio in rat urine in a dose-dependent manner in a model of 11β-hydroxysteroid dehydrogenase inhibition induced by carbenoxolone. Chronic administration 11-dehydrocorticosterone increases plasma glucocorticoids levels, body weight gain, and adiposity, as well as induces insulin resistance in mice.

Boromycin is a boron-containing macrolide antibiotic that has been found in Streptomyces. Boromycin inhibits growth of B. subtilis (MIC = 0.05 μg/ml) and induces efflux of potassium ions from B. subtilis without affecting Na+/K+-ATPase activity. It decreases the synthesis of protein, RNA, and DNA in B. subtilis when used at a concentration of 0.05 μg/ml. It inhibits the growth of B. halodurans (MIC = 10 ng/ml) and inhibits the futalosine pathway of menaquinone synthesis in B. halodurans. Boromycin (3.4 nM) reverses bleomycin-induced cell cycle arrest at the G2 phase in Jurkat cells. It inhibits replication of the HIV-1 strains LAV-1 and RF and the HIV-2 strain LAV-2 in MT-4 cells (IC50s = 0.008, 0.11, and 0.007 μM, respectively). It also inhibits replication of a clinical isolate of HIV-1, strain KK-1, in MT-4 cells and peripheral blood mononuclear cells (PBMCs; IC50s = 0.14 and <0.1 μM, respectively).

Chloroprocaine hydrochloride (Chloroprocaine HCl) is a local anesthetic during surgical procedures.

Depramine (GP 31406), a tricyclic antidepressant, exhibits pharmacological activity by inhibiting acetylcholinesterase, Mg^2+-ATPase, and Na^+/K^+ ATPase activity [1] [2].

Istaroxime, also known as PST-2744, is a positive inotropic agent that mediates its action through inhibition of sodium/potassium adenosine triphosphatase (Na+/K+ ATPase). Na+/K+ ATPase inhibition increases intracellular sodium levels, which reverses the driving force of the sodium/calcium exchanger, inhibiting calcium extrusion and possibly facilitating calcium entry. Additionally, Istaroxime increases intracellular calcium by improving the efficacy by which intracellular calcium triggers sarcoplasmic reticulum calcium release, and by accelerating the inactivation state of L-type calcium channels, which allow for calcium influx.

Actein has a stimulatory effect on osteoblastic bone formation or has potential activity against osteoporosis, it also can prevent oxidative damage to osteoblasts in osteoporotic patients. Actein's ability to pathways involved in lipid disorders and carci

Paraxanthine (1,7-dimethylxanthine) is a metabolite of caffeine (sc-202514) which functions as an adenosine receptor ligand and a PARP-1 inhibitor in pulmonary epithelial cells. Studies suggest that Paraxanthine is structurally similar to caffeine and possibly mediates the physiological effects of caffeine. Also Paraxanthine acts as a competitive phosphodiesterase inhibitor, which increases intracellular cAMP, activates PKA, inhibits TNF-α and leukotriene synthesis. In addition, Paraxanthine acts as a Na+/K+ ATPase enzymatic effector.

Odoroside H has anticancer activities, the cytotoxic effects are induced by the inhibition of the plasma membrane bound Na(+)/K(+)-ATPase.

Nepaprazole Na is the salt form of Nepaprazole Free Base, also known as TY-11345, is a proton pump inhibitor potentially for treatment of gastric ulcer. TY-11345 potently inhibited H+/K(+)-ATPase activity in isolated rabbit gastric mucosal microsomes; and the inhibitory effect was enhanced under weak acid conditions, the IC50 (concentrations that inhibit the enzyme activity by 50%) being 5.8 microM and 9.9 microM at pH 6.0 and pH 7.4, respectively. TY-11345 should be useful for the clinical treatment of peptic ulcer diseases.

Caloxin 2A1 is an inhibitor peptide of the plasma membrane Ca 2+-ATPase (PMCA) responsible for extracellular signaling. Importantly, Caloxin 2A1 has no impact on the basal Mg 2+-ATPase or Na+-K+-ATPase activities.

Germicidin A is a pyranone originally derived from S. viridochromogenes that acts as a reversible, autoregulative inhibitor of spore germination and hyphal elongation in the genus Streptomyces at concentrations as low as 200 pM. During germination, spores of Streptomyces excrete germicidin A along with other germicidin homologs, which inhibit germination of its own arthrospores. At higher concentrations, germicidin A can inhibit the porcine Na+/K+-activated ATPase (ID50 = 100 μM) and prevent the germination of the cress L. sativum.

Carsatrin is purinylpiperazine derivative. as cardiotonic and antiarrhythmic. Carsatrin acts as positive inotropic agent that increases twitch tension and prolongs the action potential (AP) duration of ventricular muscle without affecting the Na+, K+-ATPase, adenylyl cyclase, phosphodiesterase isozymes, or cardiac myofilaments. Carsatrin’s positive inotropic effect can be prevented by tetrodotoxin but not by the adrenergic antagonists timolol, yohimbine, or prazosin

ASI-254 is an aminosugar cardiac glycoside and an inhibitor of Na+,K+ -ATPase.

1. Acevaltrate (Acevaltratum) displays high cytotoxicity against GLC(4), a human small-cell lung cancer cell line, and against COLO 320, a human colorectal cancer cell line, with IC50 values of 1-6 uM.

Digitoxin (Digitoxinum) is an effective Na+/K+-ATPase inhibitor (EC50 value: 0.78 μM).

Transdermal Peptide Disulfide TFA (TD 1 Disulfide(peptide) TFA), an 11-amino acid peptide, specifically binds to the Na+/K+-ATPase beta-subunit (ATP1B1), predominantly interacting with its C-terminus. This compound is capable of enhancing the transdermal delivery of various macromolecules[1].

Wilforine is a sesquiterpene pyridine alkaloid; important bioactive compound in T. wilfordii plants, and is effective in treating idiopathic pulmonary fibrosis. Wilforine has anti-inflammatory effect, which might be mediated by down-regulation of the expr

Prilocaine (NSC-40027) is a local anesthetic of the amino amide type, which acts on the sodium channel on the neuronal membrane and limits the spread of seizures.

Chloroprocaine (2-Chloroprocaine) is an effective Na,K-ATPase activity inhibitor with an IC 50 of 13 mM. Chloroprocaine is a local anesthetics that block peripheral nerve [1].

Thujopsene, a sesquiterpene found in T. dolabrata, exhibits a wide range of biological activities. It inhibits Na+/K+-ATPase and cytochrome P450 (CYP) isoform CYP2B6 with IC50 values of 25.9 µg/ml and Ki of 0.8 µM, respectively. Additionally, thujopsene demonstrates antimicrobial efficacy against both Gram-positive and Gram-negative bacteria, such as S. aureus, M. luteus, and S. typhimurium, with MICs ranging from 25-50 µg/ml. It also suppresses antigen-induced β-hexosaminidase release in IgE-sensitized RBL-2H3 mast cells (IC50= 25.1 µM) and shows cytotoxicity against A549 non-small cell lung cancer cells with an LC50 of 35.27 µg/ml. Furthermore, thujopsene causes mortality in mites D. farinae and T. putrescentiae, with LC50s of 9.82 and 10.92 µg/cm2, respectively.

Digoxin-d3 is a deuterated compound of Digoxin. Digoxin has a CAS number of 20830-75-5. Digoxin is occasionally used in the treatment of various heart conditions, namely atrial fibrillation, atrial flutter and sometimes heart failure that cannot be controlled by other medication.

Istaroxime hydrochloride is an inhibitor of Na+/K+-ATPase (IC50: 0.11 μM). It also is a sarcoplasmic/endoplasmic reticulum calcium ATPase 2 (SERCA 2) activator.