Ion Pump Inhibitors

Ion pumps (ion transporters) are enzymes that move charged particles into or out of a cell, working against a concentration or electrochemical gradient. Ions are positively charged particles (cations) such as sodium (Na), potassium (K), and hydrogen (H) or negatively charged particles (anions) such as chloride (Cl). The ion binds to the ion pump, cause a conformational change resulting in active transport of the ion across the membrane, making them membrane transport proteins (transporters). In effect, these ion pumps convert energy from ATP, sunlight, concentration gradients, or other redox reactions to potential energy that is stored. Sigma offers several potent, selective, ion pump inhibitors that act as diuretics, antihypertentives, anesthesia, and antipoliferative or antisecretory agents.

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SML1856 8-Aminoguanine ≥95% (HPLC) 8-Aminoguanine, a guanine derivative, is an orally available and highly efficacious potassium-sparing diuretic/natriuretic that increased sodium excretion by 17.2-fold and decrease potassium excretion by 71.0%. 8-Aminoguanine increases glucose excretion by 12.1-fold. Also, 8-Aminoguanine suppressed deoxycorticosterone/salt-induced hypertension.
SML1852 8-Aminoguanosine ≥98% (HPLC) 8-Aminoguanosine is known to stimulate diuresis, natriuresis, glucosuria and antikaliuresis. It is an analog of guanosine, that can block purine nucleoside phosphorylase, in vitro and in intact lymphoid cells. 8-aminoguanosine triphosphate can be used to block GTP (guanosine triphosphate) cyclohydrolase I from human liver and Escherichia coli.
8-Aminoguanosine, a guanosine derivative, is an orally available and highly efficacious potassium-sparing diuretic/natriuretic that increased sodium excretion by 26.2-fold and decrease potassium excretion by 69.1%. 8-Aminoguanosine increases glucose excretion by 12.2-fold. Also 8-Aminoguanosine suppressed deoxycorticosterone/salt-induced hypertension.
B1793 Bafilomycin A1 from Streptomyces griseus ≥90% (HPLC) A specific inhibitor of vacuolar type H+-ATPase (V-ATPase) in animal cells, plant cells and microorganisms.
B3023 Bumetanide ≥98% Inhibitor of Na+/K+/Cl- cotransporter.
SML1360 Cariporide ≥98% (HPLC) Cariporide is a selective inhibitor of the Na+/H+ exchanger subtype 1 (NHE-1), also known as the Na+/H+ antiporter. Cariporide has shown cardioprotective and antiarrhythmic effects, and has recently been investigated for anticancer activity.
Cariporide, a sodium-hydrogen exchange inhibitor can decrease the liberation of myoglobin at the time of ischemia/reperfusion and reduces the liberation of NE (norepinephrine) during ischemia.
C8874 CGP-37157 ≥98% (HPLC), powder Specific inhibitor of mitochondrial Na+/Ca2+ exchange as well as sarcoplasmic reticulum calcium-stimulated ATPase and possibly other calcium channels.
SML0591 Chlorthalidone ≥98% (HPLC) Chlorthalidone is a thiazide-like diuretic, an inhibitor of the Na+-Cl- cotransporter. Chlorthalidone inhibits sodium ion transport across the renal tubular epithelium increasing the delivery of sodium to the distal renal tubule and indirectly increasing potassium excretion via the sodium-potassium exchange mechanism. Chlorthalidone also promotes Ca++ reabsorption by an unknown mechanism. Several recent comparison studies inidcate that chlorthalidone may be a better drug in preventing cardiovascular events than hydrochlorothiazide.
SML1368 CLP257 ≥98% (HPLC) CLP257 is a selective K+-Cl cotransporter KCC2 activator that restored impaired Cl transport in neurons with reduced KCC2 activity. Apparently, CLP257 modulates plasmalemmal KCC2 protein turnover post-translationally.
C9705 Concanamycin A ≥70% (HPLC) Cytotoxic. Inhibits acidification of organelles and perforin-mediated cytotoxicity.
D8190 3′,4′-Dichlorobenzamil hydrochloride >98% (HPLC) Inhibits Na+/Ca2+ exchanger, Na+ transport and sarcoplasmic reticulum Ca2+ release channels.
SML1766 Diphyllin ≥98% (HPLC) Diphyllin is a natural arylnaphthalene that exhibits potent anticancer and antiviral activities. Diphyllin is a potent inhibitor of vacuolar H(+)-ATPase (V-ATPase) that inhibits lysosomal acidification in osteoclasts.
SML1828 EMD-87580 ≥98% (HPLC) EMD-87580 is a selective inhibitor of the Na+/H+ exchanger subtype 1 (NHE-1), also known as the Na+/H+ antiporter. EMD-87580 has shown cardioprotective effects, and has been investigated as a possible treatment for Duchenne′s muscular dystrophy.
E7906 Esomeprazole magnesium hydrate ≥98% (HPLC) Esomeprazole magnesium dihydrate is a leading proton pump inhibitor.
SML1083 Ethacrynic acid ≥97% (HPLC) Ethacrynic acid increases the cytotoxicity of chlorambucil in rat and human tumor cell lines.
Ethacrynic acid is non sulfonamide loop diuretic that is used to treat high blood pressure and the swelling caused by diseases like congestive heart failure. Ethacrynic acid blocks sodium-potassium-chloride cotransport. Also, Ethacrynic acid potently inhibits glutathione S-transferase family members. Studies show that ethacrynic acid potently inhibits Tgase-2 (transglutaminase-2) dependent metastasis of cancer cells including lung and pancreatic cancers.
F4381 Furosemide "High ceiling" diuretic that strongly affects renal tubular action by increasing renal blood flow; antihypertensive.
Furosemide can block the Na+/K+/2Cl- co-transporter in the ascending thick loop of Henle. It can enhance the synthesis of intrarenal prostaglandin. It enhances its ototoxicity in animals when used along with kanamycin. Furosemide is linked with thiamine insufficiency in individuals with heart failure.
Inhibits ion co-transport in the kidney.
K4389 KR-32568 ≥98% (HPLC), solid Sodium/hydrogen exchanger-1 (NHE-1) inhibitor; IC50 = 0.23 μM; inhibited NHE-1-mediated rabbit platelet swelling; in anesthetized rats, reduced infarct size from 67% (control) to 43% (at 0.1 mg/kg) and 24% (at 1.0 mg/kg); reduced number of ventricular premature beats from 530 to 266 (at 0.1 mg/kg) and 115 (at 1.0 mg/kg); reduced ventricular fibrillation incidence from 17 to 8 (0.1 mg/kg) and 0 (1.0 mg/kg); implications for research and treatment of myocardial ischemic diseases.
L8533 Lansoprazole ≥98% (TLC), powder Gastric proton pump inhibitor.
SML1607 Lesinurad ≥98% (HPLC) Lesinurad is a selective inhibitor of Urate transporter 1 (URAT1), a urate-anion exchanger which is responsible for the majority of uric acid reabsorption from the renal tubular lumen. Lesinurad thus reduces serum uric acid levels. Lesinurad has been approved for use in combination with a xanthine oxidase inhibitor to treat hyperuricemia associated with gout.
O104 Omeprazole solid Omeprazole binds covalently to proton pump (H+, K+-ATPase) and inhibits gastric secretion. It is useful in ameliorating the effects of peptic oesophagitis, duodenal and gastric ulcer. Omeprazole is preferred over antagonists of histamine H2-receptor and ranitidine for its higher efficiency. It is also useful in treating Zollinger-Ellison syndrome.
O3125 Ouabain octahydrate ≥95% (HPLC), powder Cardiac glycoside, inhibits Na(+)/K(+) ATPase, regulates transcription of MDR (increase, Pgp) and MRP (increase MRP1 and decrease CFTR, cyctic fibrosis transport receptor or cAMP-activated Cl- channel) genes, also alters localization of MRP1. Ouabain resistance is associated with appearance of Na(+)/K(+) ATPase isoforms with low binding affinity.
Ouabain has its specific binding site on integral proteins of the plasma membrane. Heart disease is treated using ouabain derivatives. Increased ouabain production is observed during exercise in humans. Abnormally high levels of ouabain are indicated in congestive heart failure and hypertension. Ouabain signalling affects intracellular calcium levels, which is known to activate nuclear factor κB (NFκB).
P0021 Pantoprazole sodium hydrate ≥98% (HPLC) Pantoprazole is a benzimidazole derivative,activated in acidic environment. It is useful in treating long term prophylaxis and acid-related disorders.
Pantoprazole is a gastric proton pump inhibitor.
PZ0155 PF-03716556 ≥98% (HPLC) potent, selective and reversible acid pump antagonist (H, K-ATPase)
PZ0318 PF-06761281 ≥97% (HPLC) PF-06761281 is an inhibitor of the sodium-coupled citrate transporter (NaCT or SLC13A5), which may be a target for tretment and prevention of metabolic disorders. The SLC13 transporters SLC13A2 (NaDC1), SLC13A3 (NaDC3), and SLC13A5 (NaCT) co-transport di- and tricarboxylates with multiple sodium ions into cells. PF-06761281 inhibits citrate uptake with an IC50 of 740 nM for NaCT in human hepatocytes. PF-06761281 has >25-fold in vitro selectivity for NaCT over NaDC1 and NaDC3 and was inactive in a selectivity panel of 65 targets.
P9547 Prilocaine hydrochloride ≥98% (TLC) Used for local nerve block and for spinal anesthesia; pharmacological properties are similar to those of lidocaine.
SML0476 Rabeprazole sodium ≥98% (HPLC) Rabeprazole sodium is gastric proton pump inhibitor. It suppresses the production of acid in the stomach by inhibiting the gastric H+/K+ATPase (hydrogen-potassium adenosine triphosphatase) at the secretory surface of the gastric parietal cell. Rabeprazole sodium has been used clinically to treat acid-reflux disorders (GERD), peptic ulcer disease, H. pylori eradication, and prevent gastroinetestinal bleeds associated with NSAID use.
SML0638 S0859 ≥98% (HPLC) S0859 helps to prevent the depolarization-induced alkalinization (DIA) in astrocytes.
S0859 is a selective high-affinity generic inhibitor of the Na+/HCO3- sodium bicarbonate co-transporter (NBC). S0859 does not inhibit Na+-H+ exchange (NHE).
S5890 Sanguinarine chloride hydrate ≥98% (HPLC) A natural product with antimicrobial, anti-inflammatory, and anti-oxidant properties. Has antiproliferative, pro-apoptosis effects in some cancer cell lines.
Sanguinarine is a benzophenanthridine alkaloid isolated from plants belonging to the family Papaveracea. It exhibits anti-bacterial, anti-fungal, anti-inflammatory and anti-cancer properties. It induces cell cycle arrest and sensitizes cancer cells to apoptosis by activating TNF-related apoptosis inducing ligand.6,7 It inhibits STAT3, MMP-2, MMP-9, interacts with glutathione, induces generation of ROS, disrupts the microtubule assembly and causes DNA damage resulting the death of the cancer cells.6,7,8
S4443 SCH-28080 ≥98% (HPLC), solid SCH-28080 is a potent inhibitor of gastric H+ and K+-ATPase. The novel antiulcer agents, SCH-28080 and SCH-32651 were examined for their ability to inhibit the H+K+ ATPase enzyme activity in a preparation of microsomal membranes from rabbit fundic mucosa. SCH- 28080 inhibited the isolated enzyme activity with a potency similar to omeprazole, IC50s of 2.5 and 4.0 μM respectively. SCH 32651 was less potent exhibiting an IC50 of 200.0 μM. Both compounds may therefore exert their antisecretory activity via a direct inhibition of the parietal cell H+K+ ATPase.
S3572 Stevioside hydrate ≥98% (HPLC) Stevioside hydrate is a diterpene glycoside present in Stevia sp.
Stevioside is a noncaloric natural sweetener, 300 times more potent than sucrose. It inhibits transepithelial transport of p-aminohippurate (PAH) by interfering with the organic anion transport system. At 0.5-1 mM, it showed no interaction with any organic anion transporters (OAT).
Stevioside reportedly has genotoxic effects in cultured mammalian cells.
SML1441 Tenatoprazole ≥98% (HPLC) Tenatoprazole is a proton pump inhibitor. Tenatoprazole is an acid-activated prodrug that binds covalently to gastric H,K-ATPase, resulting in acid secretion inhibition. Tenatoprazole has a different structural class from omeprazole and most other proton pump inhibitors, with an imidazopyridine backbone rather than benzimidazole, which results in slower metabolism. Tenatoprazole thus has a long plasma half-life as compared to omeprazole, resulting in prolonged inhibition of acid secretion.
Tenatoprazole is used to maintain high diurnal and nocturnal pH levels. It prevents gastric H+,K+-ATPase with potency similar to omeprazole.
T5955 3,4,5,6-Tetrahydroxyxanthone hydrate ≥98% (HPLC) 3,4,5,6-Tetrahydroxyxanthone is a Na/K-ATPase inihibitor that inhibits pump function without activating the kinase signaling function. It inhibits Na/K ATPase pump action with an affinity comparable to ouabain, but does not alter Na or ATP affinity, is not blocked by potassium, and it does not activate the Src complex or downstream kinases.
SML0136 TGN-020 ≥98% (HPLC) TGN-020 is an inhibitor of Aquaporin 4 (AQP4), the most abundant water channel in brain. Aquaporins (AQPs) are water channels required for maintaining fluid homeostasis and enabling water movement across barrier membranes, but can enhance pathological cellular volume changes and cause edema in injury states. Pretreatment with the AQP4 inhibitor TGN-020 significantly reduced the volume of brain edema associated with ischemic injury in a mouse model of focal cerebral ischemia.
T3202 Torsemide ≥98% (HPLC), solid Torsemide functions in the thick ascending limb of the loop of Henle and enhances the excretion of sodium, chloride and water from the luminal side of the cells. Furthermore, torsemide can treat oedematous conditions that are associated with diseases such as liver cirrhosis, kidney disorders and chronic congestive heart failure2.
Torsemide is a loop diuretic of the pyridine-sulfonylurea class with antialdosteronergic properties and inhibitor of the Na+/K+/2Cl- carrier system.
V3890 VU0240551 ≥98% (HPLC) VU0240551 is a potent, selective KCC2 inhibitor. KCC2 is a potassium-chloride exchanger expressed specifically in neurons. KCC2 functions to lower intracellular chloride concentrations below the electrochemical potential of the cells, thereby increasing the hyperexcitability of the neurons. KCC2 activity enhances GABA and other inhibitory neurotransmission and is implicated in pain processing. VU0240551 was discovered in a high-throughput screen, followed by directed medicinal chemistry. VU0240551 is selective for KCC2 over NKCC1. VU0240551 binds competitively to the K+ site and binds noncompetitively to the Cl- site. VU0240551 is the only small molecule with specificity for a KCC family member.
SML0915 Xipamide ≥98% (HPLC) Xipamide is a sulfonamide diuretic that blocks sodium reabsorption in the distal tubules of the kidney, resulting in increased urine output. Xiopamide also blocks the cystic fibrosis transmembrane conductance regulator (CFTR) chloride channel.
SML0076 Zoniporide hydrochloride hydrate ≥98% (HPLC) Zoniporide is a potent and selective inhibitor of Na+/H+ exchanger isoform 1 (NHE-1). IC50 = 59 nM at NHE-1, vs. 12,000 nM at NHE-2; Zoniporide inhibits NHE-1-dependent Na+ update with IC50 of 14 nM.
Zoniporide, a selective inhibitor of sodium-hydrogen exchanger isoform 1 (NHE-1) has cardioprotective effects against myocardial injuries and ischemic insults. It inhibits the swelling human platelets and attenuates cardiac contractile dysfunction in rats. Zoniporide might have neurotoxic effects as it causes peripheral sensory axonopathy.