Na-K-ATPase-Inhibitors-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/Na+_K+ ATPase.html Na+/K+ HYPERLINK https:/www.MedChemE/Targets/Na+_K+ ATPase.html HYPERLINK https:/www.MedChemE/Targets/Na+_K+ ATPase.html ATPaseSodium potassium pumpNa+/K+ ATPase (Sodium potassium pump) is a transmembrane protein complex found in all higher e

2、ukaryotes acting as a keyenergy-consuming pump maintaining ionic and osmotic balance in cells. Na+/K+ ATPase is an emerging cancer target that meritsfurther investigation.The constant activity of the Na+/K+-ATPase (NKA, or Na+ pump) is essential for re-establishing and maintaining this gradient. Inc

3、ardiac and vascular smooth muscle the principal isoforms of the NKA are 1 and 2 and their physiological role is controlled bothby their unique and independent signalling pathways, and their discrete subcellular distribution.www.MedChemE 1 HYPERLINK https:/www.MedChemE/Targets/Na+/K+ ATPase.html Na+/

4、K+ HYPERLINK https:/www.MedChemE/Targets/Na+/K+ ATPase.html HYPERLINK https:/www.MedChemE/Targets/Na+/K+ ATPase.html ATPase HYPERLINK https:/www.MedChemE/Targets/Na+/K+ ATPase.html HYPERLINK https:/www.MedChemE/Targets/Na+/K+ ATPase.html Inhibitors, HYPERLINK https:/www.MedChemE/Targets/Na+/K+ ATPas

5、e.html HYPERLINK https:/www.MedChemE/Targets/Na+/K+ ATPase.html Antagonists, HYPERLINK https:/www.MedChemE/Targets/Na+/K+ ATPase.html HYPERLINK https:/www.MedChemE/Targets/Na+/K+ ATPase.html Activators HYPERLINK https:/www.MedChemE/Targets/Na+/K+ ATPase.html HYPERLINK https:/www.MedChemE/Targets/Na+

6、/K+ ATPase.html & HYPERLINK https:/www.MedChemE/Targets/Na+/K+ ATPase.html HYPERLINK https:/www.MedChemE/Targets/Na+/K+ ATPase.html Modulators HYPERLINK https:/www.MedChemE/_addition_-SJ733.html (+)-SJ733(SJ000557733) Cat. No.: HY-19556 HYPERLINK https:/www.MedChemE/Acevaltrate.html AcevaltrateCat.

7、No.: HY-N2070(+)-SJ733 is an anti-malaria agent which canalso inhibit Na+-ATPase PfATP4.Acevaltrate inhibits the Na+/K+-ATPaseactivity in the rat kidney and brain hemisphereswith IC s of 22.8 M and 42.3 M, respectively.50Purity: 99.45%Clinical Data: No Development ReportedSize: 1 mg, 5 mg, 10 mg, 50

8、 mg, 100 mgPurity: 99.88%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/annonacin.html Annonacin HYPERLINK https:/www.MedChemE/annonacin.html HYPERLINK https:/www.MedChemE/antimalarial-agent-7.html Antimalarial HYPERLINK https:

9、/www.MedChemE/antimalarial-agent-7.html HYPERLINK https:/www.MedChemE/antimalarial-agent-7.html agent HYPERLINK https:/www.MedChemE/antimalarial-agent-7.html HYPERLINK https:/www.MedChemE/antimalarial-agent-7.html 7Cat. No.: HY-N2877 Cat. No.: HY-145327Annonacin is an Acetogenin and promotescytotoxi

10、city via a pathway inhibiting themitochondrial complex. Annonacin is the activeagent found in Graviola leaf extract to act as aninhibitor of sodium/potassium (NKA) andsarcoplasmic reticulum (SERCA) ATPase pumps.Antimalarial agent 7 is a potent inhibitor ofPfATP4. PfATP4 is an essential ion pump on t

11、heparasite surface. Antimalarial agent 7 has thepotential for the research of human malariaparasite, Plasmodium falciparum.Purity: 97.0%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/bafilomycin-c1

12、.html Bafilomycin HYPERLINK https:/www.MedChemE/bafilomycin-c1.html HYPERLINK https:/www.MedChemE/bafilomycin-c1.html C1Cat. No.: HY-130173 HYPERLINK https:/www.MedChemE/biacetyl-monoxime.html Biacetyl HYPERLINK https:/www.MedChemE/biacetyl-monoxime.html HYPERLINK https:/www.MedChemE/biacetyl-monoxi

13、me.html monoxime(Diacetyl monoxime; DAM) Cat. No.: HY-Y0413Bafilomycin C1 is a macrolide antibiotic isolatedfrom Streptomyces sp. Bafilomycin C1 is apotent, specific and reversible inhibitor ofvacuolar-type H+-ATPases (V-ATPases). BafilomycinC1 inhibits growth of gram-positive bacteria andfungi.Biac

14、etyl monoxime (Diacetyl monoxime), a myosinATPase inhibitor, is a skeletal and cardiacmuscle contraction inhibitor. Biacetyl monoximeinduces sarcoplasmic reticulum Ca2+ release.Purity: 99.0%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1

15、00 mg HYPERLINK https:/www.MedChemE/Bufalin.html Bufalin HYPERLINK https:/www.MedChemE/Bufalin.html HYPERLINK https:/www.MedChemE/chloroprocaine-hydrochloride.html Chloroprocaine HYPERLINK https:/www.MedChemE/chloroprocaine-hydrochloride.html HYPERLINK https:/www.MedChemE/chloroprocaine-hydrochlorid

16、e.html hydrochlorideCat. No.: HY-N0877(2-Chloroprocaine hydrochloride) Cat. No.: HY-B1604Bufalin is an active component isolated from ChanSu, acts as a potent Na+/K+-ATPase inhibitor,binds to the subunit 1, 2 and 3, with K ofd42.5, 45 and 40 nM, respectively. Anti-canceractivity.Chloroprocaine hydro

17、chloride (2-Chloroprocainehydrochloride) is a potent inhibitor ofNa,K-ATPase activity with an IC of 13 mM.50Chloroprocaine hydrochloride blocks peripheralnerve.Purity: 99.86%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mgPurity: 99.18%Clinical Data: LaunchedSize: 10 mM 1 mL, 5 mg

18、, 10 mg, 25 mg, 100 mg HYPERLINK https:/www.MedChemE/Chlorpropamide.html Chlorpropamide HYPERLINK https:/www.MedChemE/Chlorpropamide.html HYPERLINK https:/www.MedChemE/citreoviridin.html CitreoviridinCat. No.: HY-B1429 Cat. No.: HY-N6745Chlorpropamide is an oral antihyperglycemic agentused for the t

19、reatment of non-insulin-dependentdiabetes mellitus (NIDDM). Target: Chlorpropamidebelongs to the sulfonylurea class of insulinsecretagogues, which act by stimulating cells ofthe pancreas to release insulin.Citreoviridin, a toxin from Penicilliumcitreoviride NRRL 2579, inhibits brain synaptosomalNa+/

20、K+-ATPase whereas in microsomes, bothNa+/K+-ATPase and Mg2+-ATPase activitiesare significantly stimulated in a dose-dependentmanner.Purity: 99.58%Clinical Data: LaunchedSize: 10 mM 1 mL, 500 mgPurity: 99.65%Clinical Data: No Development ReportedSize: 1 mg2 Tel: 609-228-6898 Fax: 609-228-5909 Email:

21、salesMedChemE HYPERLINK https:/www.MedChemE/deslanoside.html Deslanoside(Deacetyllanatoside C; Desacetyllanatoside C) Cat. No.: HY-A0154 HYPERLINK https:/www.MedChemE/Digitoxin.html DigitoxinCat. No.: HY-B1357Deslanoside (Desacetyllanatoside C) is a rapidlyacting cardiac glycoside used to treat cong

22、estiveheart failure and supraventricular arrhythmias dueto reentry mechanisms, and to control ventricularrate in the treatment of chronic atrialfibrillation.Digitoxin is an effective Na+/K+-ATPase inhibitor,the EC50 value of Digitoxin is 0.78 M.Purity: 99.76%Clinical Data: LaunchedSize: 10 mM 1 mL,

23、5 mg, 10 mgPurity: 99.36%Clinical Data: LaunchedSize: 10 mM 1 mL, 5 mg HYPERLINK https:/www.MedChemE/digoxigenin-monodigitoxoside.html Digoxigenin HYPERLINK https:/www.MedChemE/digoxigenin-monodigitoxoside.html HYPERLINK https:/www.MedChemE/digoxigenin-monodigitoxoside.html monodigitoxosideCat. No.:

24、 HY-145154 HYPERLINK https:/www.MedChemE/Ginsenoside-Rb1.html Ginsenoside HYPERLINK https:/www.MedChemE/Ginsenoside-Rb1.html HYPERLINK https:/www.MedChemE/Ginsenoside-Rb1.html Rb1(Gypenoside III) Cat. No.: HY-N0039Digoxigenin monodigitoxoside is a Na+/K+ ATPaseinhibitor and cardiac glycoside metabol

25、ite ofdigoxin.Ginsenoside Rb1, a main constituent of the root ofPanax ginseng, inhibits Na+, K+-ATPaseactivity with an IC of 6.31.0 M. Ginsenoside50also inhibits IRAK-1 activation and phosphorylationof NF-B p65 .Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98.75%Clinical

26、Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/gitoxin.html GitoxinCat. No.: HY-136933 HYPERLINK https:/www.MedChemE/Istaroxime.html Istaroxime(PST2744) Cat. No.: HY-15718Gitoxin, a Na+/K+-ATPase inhibitor, usuallyappears as a result of

27、 metabolic degradation ofDigitoxin, is just the hydroxyl (ZOH) group closeto the C-17 position, which changes thepharmacokinetics and pharmacodynamics of thesesubstances considerably.Istaroxime (PST2744) is a potent inhibitor ofNa+,K+-ATPase with IC of 0.11 M.50Purity: 98%Clinical Data: No Developme

28、nt ReportedSize: 5 mgPurity: 98%Clinical Data: Phase 2Size: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/Istaroxime-hydrochloride.html Istaroxime HYPERLINK https:/www.MedChemE/Istaroxime-hydrochloride.html HYPERLINK https:/www.MedChemE/Istaroxime-hydrochloride.html hydrochloride HYPERLINK https:/www.Med

29、ChemE/Istaroxime-hydrochloride.html HYPERLINK https:/www.MedChemE/marinobufogenin.html Marinobufogenin(PST2744 hydrochloride) Cat. No.: HY-15718ACat. No.: HY-N6574Istaroxime hydrochloride is a Na+/K+-ATPaseinhibitor (IC =0.11 M) and a50sarcoplasmic/endoplasmic reticulum calcium ATPase2 (SERCA 2) act

30、ivator.Marinobufogenin is a strong inhibitor of Na+/K+ATPase that has been identified in mammalianplasma.Purity: 99.32%Clinical Data: Phase 2Size: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 99.89Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/neriifolin.html N

31、eriifolin HYPERLINK https:/www.MedChemE/neriifolin.html HYPERLINK https:/www.MedChemE/Oleandrin.html Oleandrin(17-Neriifolin) Cat. No.: HY-N8441 (PBI-05204) Cat. No.: HY-13719Neriifolin, a CNS-penetrating cardiac glycoside,is an inhibitor of the Na+, K+-ATPase.Neriifolin can target beclin 1, inhibit

32、s theformation of LC3-associated phagosomes andameliorates experimental autoimmuneencephalomyelitis (EAE) development.Oleandrin (PBI-05204) inhibits the Na+,K+-ATPase activity with an IC of 620 nM.50Purity: 96.0%Clinical Data: No Development ReportedSize: 5 mgPurity: 99.44%Clinical Data: Phase 2Size

33、: 10 mM 1 mL, 2 mg, 5 mg, 10 mg, 25 mgwww.MedChemE 3 HYPERLINK https:/www.MedChemE/Oleic_acid.html Oleic HYPERLINK https:/www.MedChemE/Oleic_acid.html HYPERLINK https:/www.MedChemE/Oleic_acid.html acid(9-cis-Octadecenoic acid; 9Z-Octadecenoic acid) Cat. No.: HY-N1446 HYPERLINK https:/www.MedChemE/ol

34、eic-acid-13c.html Oleic HYPERLINK https:/www.MedChemE/oleic-acid-13c.html HYPERLINK https:/www.MedChemE/oleic-acid-13c.html acid-13C(9-cis-Octadecenoic acid-13C; 9Z-Octadecenoic acid-13C) Cat. No.: HY-N1446SOleic acid (9-cis-Octadecenoic acid) is anabundant monounsaturated fatty acid. Oleic acid isa

35、 Na+/K+ ATPase activator.Oleic acid-13C (9-cis-Octadecenoic acid-13C) isthe 13C labeled Oleic acid. Oleic acid(9-cis-Octadecenoic acid) is an abundantmonounsaturated fatty acid. Oleic acid is aNa+/K+ ATPase activator.Purity: 98.0%Clinical Data: LaunchedSize: 10 mM 1 mL, 1 mg, 5 mg, 10 mgPurity: 98%C

36、linical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/oleic-acid-13c-1.html Oleic HYPERLINK https:/www.MedChemE/oleic-acid-13c-1.html HYPERLINK https:/www.MedChemE/oleic-acid-13c-1.html acid-13C-1Cat. No.: HY-N1446S4 HYPERLINK https:/www.MedChemE/oleic-acid-13c18.html O

37、leic HYPERLINK https:/www.MedChemE/oleic-acid-13c18.html HYPERLINK https:/www.MedChemE/oleic-acid-13c18.html acid-13C18 HYPERLINK https:/www.MedChemE/oleic-acid-13c18.html (9-cis-Octadecenoic acid-13C18;9Z-Octadecenoic acid-13C18) Cat. No.: HY-N1446S2Oleic acid-13C-1 is the 13C labeled Oleic acid.Ol

38、eic acid (9-cis-Octadecenoic acid) is anabundant monounsaturated fatty acid. Oleic acid isa Na+/K+ ATPase activator.Oleic acid-13C18 (9-cis-Octadecenoic acid-13C18)is the 13C labeled Oleic acid. Oleic acid(9-cis-Octadecenoic acid) is an abundantmonounsaturated fatty acid. Oleic acid is aNa+/K+ ATPas

39、e activator.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/oleic-acid-d17.html Oleic HYPERLINK https:/www.MedChemE/oleic-acid-d17.html HYPERLINK https:/www.MedChemE/oleic-acid-d17.html a

40、cid-d17(9-cis-Octadecenoic acid-d17; 9Z-Octadecenoic acid-d17) Cat. No.: HY-N1446S3 HYPERLINK https:/www.MedChemE/oleic-acid-d2.html Oleic HYPERLINK https:/www.MedChemE/oleic-acid-d2.html HYPERLINK https:/www.MedChemE/oleic-acid-d2.html acid-d2(9-cis-Octadecenoic acid-d2; 9Z-Octadecenoic acid-d2) Ca

41、t. No.: HY-N1446S1Oleic acid-d17 (9-cis-Octadecenoic acid-d17) isthe deuterium labeled Oleic acid. Oleic acid(9-cis-Octadecenoic acid) is an abundantmonounsaturated fatty acid. Oleic acid is aNa+/K+ ATPase activator.Oleic acid-d2 (9-cis-Octadecenoic acid-d2) is thedeuterium labeled Oleic acid. Oleic

42、 acid(9-cis-Octadecenoic acid) is an abundantmonounsaturated fatty acid. Oleic acid is aNa+/K+ ATPase activator.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/Ouabain-Octahydrate.html Ou

43、abain HYPERLINK https:/www.MedChemE/Ouabain-Octahydrate.html HYPERLINK https:/www.MedChemE/Ouabain-Octahydrate.html Octahydrate HYPERLINK https:/www.MedChemE/Ouabain-Octahydrate.html HYPERLINK https:/www.MedChemE/Phlorizin.html Phlorizin(Acocantherine; G-Strophanthin) Cat. No.: HY-B0542 (Floridzin;

44、NSC 2833) Cat. No.: HY-N0143Ouabain Octahydrate is an inhibitor ofNa+/K+-ATPase, used for the treatment ofcongestive heart failure.Phlorizin is a non-selective SGLT inhibitor withKis of 300 and 39 nM for hSGLT1 and hSGLT2,respectively. Phlorizin is also a Na+/K+-ATPaseinhibitor.Purity: 99.96%Clinica

45、l Data: LaunchedSize: 10 mM 1 mL, 100 mgPurity: 99.82%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 500 mg, 1 g, 5 g HYPERLINK https:/www.MedChemE/prilocaine.html Prilocaine HYPERLINK https:/www.MedChemE/prilocaine.html HYPERLINK https:/www.MedChemE/prilocaine-hydrochloride.html Prilocaine

46、 HYPERLINK https:/www.MedChemE/prilocaine-hydrochloride.html HYPERLINK https:/www.MedChemE/prilocaine-hydrochloride.html hydrochlorideCat. No.: HY-B0137 Cat. No.: HY-B0137APrilocaine, an amino amide, is a Na, K-ATPaseinhibitor. Prilocaine has neurotoxic effects.Prilocaine hydrochloride, an amino ami

47、de, is aNa, K-ATPase inhibitor. Prilocaine hasneurotoxic effects.Purity: 99.03%Clinical Data: LaunchedSize: 10 mM 1 mL, 50 mg, 100 mgPurity: 98%Clinical Data: LaunchedSize: 5 mg, 10 mg, 25 mg4 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/prilocaine-d7-hydroc

48、hloride.html Prilocaine-d7 HYPERLINK https:/www.MedChemE/prilocaine-d7-hydrochloride.html HYPERLINK https:/www.MedChemE/prilocaine-d7-hydrochloride.html hydrochlorideCat. No.: HY-B0137AS HYPERLINK https:/www.MedChemE/Rostafuroxin.html Rostafuroxin(PST 2238) Cat. No.: HY-12283Prilocaine-d7 (hydrochlo

49、ride) is deuterium labeledPrilocaine (hydrochloride). Prilocainehydrochloride, an amino amide, is a Na, K-ATPaseinhibitor. Prilocaine has neurotoxic effects.Rostafuroxin (PST 2238), a digitoxigeninderivative, is an orally active and potentNa+,K+-ATPase (ATP1A1) antognist.Purity: 98%Clinical Data: No

50、 Development ReportedSize: 1 mg, 5 mgPurity: 98.07%Clinical Data: Phase 2Size: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/sodium-oleate.html Sodium HYPERLINK https:/www.MedChemE/sodium-oleate.html HYPERLINK https:/www.MedChemE/sodium-oleate.html oleate HYPERLINK https:/www.

51、MedChemE/sodium-oleate.html (Oleic acid sodium; 9-cis-Octadecenoic acidsodium; 9Z-Octadecenoic acid sodium) Cat. No.: HY-N1446B HYPERLINK https:/www.MedChemE/strophanthidin.html StrophanthidinCat. No.: HY-114252Sodium oleate (Oleic acid sodium) is an abundantmonounsaturated fatty acid sodium. Sodium oleateis a Na+/K+ ATPase activator.Strophanthidin is a naturally available cardiacglycoside. Strophanthidin 0.1 and 1 nmol/Lincreases and 1100 mol/L inhi