Shop By
Catalog No.
Product Name
Application
Product Information
Citations
-
NCX Inhibitor
YM-244769 is a potent and selective inhibitor of the Na+/Ca2+ exchanger (NCX), primarily targeting NCX3. With IC50 values of 18 nM and 50 nM for inhibiting the unidirectional outward NCX current, it effectively reduces Ca2+ entry. This compound has demonstrated protective effects against hypoxia/reoxygenation-induced damage in SH-SY5Y neuronal cells and has been shown to increase urine volume and urinary electrolyte excretion in murine models, making it valuable for studies related to cellular stress responses and fluid regulation. -
NCX Inhibitor
YM-244769 dihydrochloride is a selective and orally active inhibitor of the Na+/Ca2+ exchanger (NCX), particularly targeting the NCX3 isoform. With IC50 values of 18 nM for NCX3, it effectively suppresses outward NCX currents, facilitating studies on calcium signaling in neurons. This compound demonstrates protective effects against hypoxia/reoxygenation-induced damage in SH-SY5Y neuronal cells, making it a valuable reagent for research in neuroprotection and related fields. Additionally, it has been shown to influence urinary output and electrolyte excretion in mouse models, contributing to its utility in pharmacological studies. -
NCX Inhibitor
YM-244769 hydrochloride is a selective inhibitor of the Na+/Ca2+ exchanger (NCX), primarily targeting NCX3. With IC50 values of 18 nM and 50 nM for inhibiting the outward NCX current and Ca2+ entry mode, respectively, it demonstrates significant potential in neuroprotection, effectively mitigating hypoxia/reoxygenation-induced damage in SH-SY5Y neuronal cells. Additionally, YM-244769 hydrochloride has been shown to enhance urine volume and promote urinary excretion of electrolytes in murine models. -
Sodium-Calcium Exchanger Inhibitor
KB-R7943 is a selective inhibitor of the sodium-calcium exchanger, exhibiting an IC50 value of 5.1 µM. This compound is utilized as a valuable tool in studies involving cardiac and renal failure models, facilitating research into calcium homeostasis and its implications in heart and kidney function. -
Sodium Channel Inhibitor
Benzamil is a sodium channel inhibitor, functioning as a non-selective blocker of epithelial sodium channels (ENaC) and a Na+/Ca2+ exchanger (NCX) inhibitor with an IC50 value of approximately 100 nM. Its pharmacological properties include the enhancement of myogenic vasoconstriction. Additionally, Benzamil inhibits TRPP3-mediated Ca2+-activated currents, exhibiting an IC50 of 1.1 μM. This compound is valuable for research applications focused on cardiovascular physiology and electrolyte transport mechanisms. -
Na+/Ca2+ exchanger (NCX) Inhibitor
SAR296968 is a selective inhibitor of the Na+/Ca2+ exchanger (NCX), demonstrating an IC50 value of 74 nM against human NCX1. It effectively inhibits both forward and reverse modes of NCX activity, leading to enhanced cardiac contractility and increased stroke volume. Additionally, SAR296968 exhibits antiarrhythmic properties, making it valuable for research focused on heart failure and related cardiovascular conditions. -
NCX Inhibitor
NCX1-IN-1 is a potent inhibitor of the Na+/Ca2+ exchanger (NCX), a critical regulator of intracellular calcium levels. By specifically targeting NCX, this compound is instrumental in studying calcium homeostasis and related signaling pathways. NCX1-IN-1 is valuable for research applications focused on cardiovascular diseases, neurodegenerative disorders, and cellular stress responses. -
H+/K+-ATPase Inhibitor
DBM-819 is a reversible inhibitor of H⁺/K⁺-ATPase, exhibiting an IC50 value of 5 µM. This compound effectively inhibits gastric acid secretion by blocking the proton pump in the gastric mucosa, demonstrating significant protective effects against duodenal ulcers induced by Cysteamine, and gastric ulcers induced by Indomethacin and Aspirin, with EC50 values of 6, 3.1, and 4 mg/kg, respectively. DBM-819 serves as a valuable tool in research focused on ulcer prevention and gastroprotection. -
H+/K+-ATPase Inhibitor
ATPase-IN-7 is a potent inhibitor of H+/K+-ATPase, which plays a crucial role in regulating gastric acid secretion. This compound is primarily utilized in research focused on gastrointestinal inflammatory diseases and conditions related to gastric acidity. Its inhibitory effect makes it a valuable tool for studying acid-related pathologies and potential therapeutic interventions. -
Na+/K+ ATPase Inhibitor
Acevaltrate is a selective inhibitor of Na+/K+ ATPase, demonstrating IC50 values of 22.8 μM in rat kidney tissues and 42.3 μM in brain hemispheres. This compound is valuable for studying ion transport mechanisms and the physiological roles of Na+/K+ ATPase in renal and neurological contexts. Its inhibitory effects make it a suitable tool for exploring potential therapeutic applications in conditions related to dysregulated ion homeostasis. -
Na, K-ATPase Inhibitor
Digoxigenin monodigitoxoside is an inhibitor of Na,K-ATPase and a metabolite of Digoxin. It modulates cardiac function by affecting ion transport, making it valuable for studying cardiovascular diseases, including congestive heart failure and cardiac arrhythmias. This reagent is essential for researchers investigating the mechanisms of cardiac glycosides and their therapeutic potential. -
Na+/K+-ATPase Inhibitor
Gitoxin is a potent Na+/K+-ATPase inhibitor that significantly alters cellular ion homeostasis. It is a metabolite derived from the degradation of Digitoxin, featuring a hydroxyl (ZOH) group at the C-17β position, which impacts its pharmacokinetic and pharmacodynamic properties. Gitoxin's inhibitory effect on Na+/K+-ATPase makes it a valuable tool in cardiovascular research and studies involving ion transport mechanisms. -
Na+/K+ ATPase Inhibitor
Marinobufogenin is a potent Na+/K+ ATPase inhibitor found in mammalian plasma. It exhibits significant biological activity by modulating electrolyte balance and influencing cellular signaling pathways. Research applications include studies on cardiovascular function, renal physiology, and the exploration of cellular mechanisms related to ion transport. -
Na+/K+ ATPase Inhibitor
Transdermal Peptide Disulfide is a synthetic 11-amino acid peptide that serves as an inhibitor of the Na+/K+-ATPase by binding to the beta-subunit (ATP1B1) and specifically interacting with its C-terminus. This compound enhances the transdermal delivery of various macromolecules, making it a valuable tool in drug formulation and transdermal research applications. Its ability to facilitate the transport of biologically relevant molecules may have significant implications for improving therapeutic delivery in clinical settings. -
Na, K-ATPase Inhibitor
Prilocaine hydrochloride is an amino amide that functions as an inhibitor of Na+/K+-ATPase. This compound exhibits neurotoxic properties, making it relevant for studies involving neuronal function and toxicity. Research applications include exploring membrane transport mechanisms and assessing the impacts of ion channel modulation on cellular activity. -
Na+/K+ ATPase Inhibitor
Stauntosaponin A is a steroid glycoside that serves as a potent inhibitor of Na+/K+ ATPase, demonstrating an IC50 value of 21 nM. Isolated from Carnation, this compound exhibits significant biological activity that may be leveraged in anti-cancer research. Its ability to modulate ion transport makes it a valuable tool for exploring cellular mechanisms and therapeutic interventions in cancer biology. -
Na+/K+ ATPase Inhibitor
Suloctidil hydrochloride is a potent Na+/K+ ATPase inhibitor that modulates membrane fluidity in rat brain synaptosomes. It demonstrates significant biological activity relevant to neurological research and is under investigation in clinical trials for potential therapeutic applications in dementia and thrombotic disorders. -
ATPase Inhibitor
16-HETE is an arachidonic acid metabolite that functions primarily as an ATPase inhibitor. It demonstrates vasodilatory effects and inhibits polymorphonuclear leukocyte (PMN) activity, making it valuable in studying inflammatory processes. Additionally, 16-HETE serves as a biomarker in the early detection of non-alcoholic fatty liver disease, facilitating research into metabolic disorders and their progression. -
H⁺/K⁺ ATPase Inhibitor
AU-461 is a reversible inhibitor of the gastric H⁺/K⁺ ATPase, exhibiting IC₅₀ values of 12.15 μM for rabbit-derived enzymes and 4.20 μM for pig-derived enzymes. By competing with activated cationic K⁺ (Kᵢ = 1.64 μM), AU-461 effectively reduces both histamine-stimulated and basal gastric acid secretion in rat models. This compound demonstrates protective effects against ulcer formation induced by ethanol or sodium hydroxide and normalizes plasma gastrin levels. AU-461 is valuable for research into the mechanisms of peptic ulcers and gastric acid regulation. -
Na+/K+ ATPase inhibitor
Ro 18-5364 is a selective inhibitor of gastric H+/K+ ATPase, primarily targeting the enzyme's activity. It demonstrates significant inhibition, particularly at lower pH levels, making it a valuable tool for studying gastric physiology. The compound's effects on enzyme activity, proton transport, and binding interactions can be assessed through various experimental methodologies, providing insights into its mechanism of action and potential therapeutic applications in conditions related to proton pump regulation. -
Na+/K+ ATPase Inhibitor
AR-HO47108 is a reversible inhibitor of the Na+/K+ ATPase, primarily targeting the potassium ion binding site within gastric wall cells. By competitively blocking this site, AR-HO47108 effectively reduces gastric acid secretion, making it a valuable tool for investigating conditions associated with excessive gastric acid, such as peptic ulcers. This compound is particularly useful for research into gastric physiology and related gastrointestinal disorders. -
Cation ATPases Inhibitor
SPAI-1 is a specific inhibitor of monovalent cation transporting ATPases, targeting Na+, K+-ATPase and H+, K+-ATPase to provide valuable insights into ionic transport mechanisms. Isolated from porcine duodenum, SPAI-1 demonstrates the ability to inhibit these ATPases in vitro while also stimulating Mg2+-ATPase activity. This compound is essential for research applications involving cellular ion homeostasis and ATPase-related signaling pathways. -
Na+/K+-ATPase Inhibitor
14-Anhydrodigitoxigenin is a potent inhibitor of Na+/K+-ATPase, a crucial enzyme involved in maintaining ion gradients across cell membranes. Derived from the leaves of Acokanthera oblongifolia, this cardenolide exhibits significant biological activity relevant to cardiovascular research and cellular physiology. Its application in studies of cardiac function and electrolyte balance makes it a valuable reagent for investigating the roles of Na+/K+-ATPase in various physiological and pathological processes. -
Na+/K+ ATPase Inhibitor
LND 623 is a Na+/K+ ATPase inhibitor known for its positive inotropic effects. This aminosteroid compound effectively inhibits Na+/K+ ATPase activity, making it a valuable tool in cardiovascular research. With an LD50 of approximately 45 mg/kg when administered intravenously, LND 623 presents a significantly higher tolerance compared to ouabain, facilitating studies in cardiac function and related therapies. -
Proton Pump Inhibitor
A 80915A is a potent proton pump inhibitor derived from seminaphthoquinone, which is produced by the Streptomyces species. It functions primarily by inhibiting Na+/K+ ATPase, a key enzyme involved in gastric acid secretion. This compound is valuable for research applications focused on understanding gastrointestinal physiology and exploring therapeutic strategies for acid-related disorders. -
Na+/K+ ATPase Inhibitor
Laurinterol is a potent inhibitor of the Na+/K+-ATPase sodium-potassium ion pump. Isolated from Laurencia johnstonii, Laurinterol disrupts ion transport, influencing cellular homeostasis and signaling pathways. This compound is useful in research related to electrolyte balance, cellular physiology, and neurobiology, providing insights into the role of ion pumps in various biological processes. -
Na+/K+ ATPase Inhibitor
Istaroxime oxalate is a Na+/K+ ATPase inhibitor, functioning as an inotropic agent with an IC50 of 0.11 μM. This reagent enhances the force of contraction in guinea pig atria and increases twitch amplitude in isolated guinea pig myocytes, demonstrating significant potential for cardiac function studies. Its ability to exert these effects without inducing lethal arrhythmias makes it valuable for research in cardiovascular physiology and pharmacology. -
H+/K+ ATPase Inhibitor
SK&F 97574 hydrochloride is a reversible inhibitor of the H+/K+ ATPase enzyme, demonstrating significant efficacy in reducing gastric acid secretion. Its primary biological activity supports the healing of acid-related upper gastrointestinal ulcers, making it valuable for research into gastrointestinal disorders and acid secretion regulation. This reagent is essential for studies focused on the pharmacological modulation of gastric acid dynamics. -
Na+/K+ ATPase Inhibitor
Rs-029 is a selective inhibitor of Na+/K+ ATPase and an activator of Mg2+ ATPase. It effectively reduces ATP levels in red blood cells, which can be critical for studying energy metabolism and ion balance in cellular systems. This compound is valuable for research applications focused on membrane transport mechanisms and investigating cellular responses to altered energy states. -
Adenosine reuptake inhibitor
Dilazep dihydrochloride is an adenosine uptake inhibitor that promotes vasodilation in cerebral and coronary circulation by enhancing the effects of adenosine. This compound exhibits protective properties against ischemic damage, reduces platelet aggregation, and interferes with the membrane transport of nucleosides. It is valuable in research applications focused on cardiovascular physiology and neurological protection. -
human ENT4 inhibitor
hENT4-IN-1 is a selective inhibitor of the human equilibrative nucleoside transporter 4 (ENT4), exhibiting an IC50 of 74.4 nM. This compound is crucial for investigating the biological roles of ENT4 in cellular nucleoside transport and metabolism. Its application extends to studies evaluating the impact of ENT4 inhibition on various physiological and pathological processes, making it a valuable tool for research in cancer biology and therapeutic development. -
ENT2 Inhibitor
FPMINT is a potent, irreversible, and non-competitive inhibitor of Equilibrative Nucleoside Transporters (ENTs), with a higher selectivity for ENT2 compared to ENT1. By effectively blocking ENT2, FPMINT significantly impacts uridine uptake, making it a valuable tool in studies related to nucleoside transport mechanisms. Its application in research can aid in elucidating the physiological roles of ENT2 in various biological processes. -
Adenosine reuptake inhibitor
Dilazep is an adenosine uptake inhibitor that enhances the effects of adenosine, leading to cerebral and coronary vasodilation. This compound not only reduces ischemic damage but also inhibits platelet aggregation and the membrane transport of nucleosides. Dilazep is useful in research applications focused on cardiovascular physiology and neuroprotection. -
hCNT1 Inhibitor
dMeThPmR is a selective inhibitor of the human nucleoside transporter 1 (hCNT1), exhibiting a potent inhibitory constant (Ki) in the range of 0.3-0.98 μM. While dMeThPmR shows minimal inhibition of hCNT2 (IC50 = 133 μM) and hCNT3 (Ki = 32.7 μM), it effectively protects cells from the cytotoxic effects of nucleoside drugs. This compound is valuable for research on cancer and related therapies, providing insights into nucleoside transport mechanisms and drug interactions. -
hCNT1 Inhibitor
MeThPmR is a potent and selective inhibitor of the human nucleoside transporter 1 (hCNT1) with a Ki ranging from 0.16 to 0.69 μM. It exhibits minimal inhibitory activity on hCNT2 (IC50 = 360 μM) and hCNT3 (Ki = 4.7 μM). MeThPmR has been demonstrated to provide protection against the cytotoxic effects of nucleoside drugs, making it a valuable tool for cancer research applications. -
P-glycoprotein Inhibitor
NSC 23925B is a potent inhibitor of P-glycoprotein (P-gp), which plays a critical role in multidrug resistance in cancer cells. This compound effectively reverses P-glycoprotein-mediated resistance and shows moderate inhibitory activity against CYP2B6 and CYP2D6 with IC50 values of 8.589 μM and 1.407 μM, respectively. NSC 23925B is valuable for research focused on overcoming multidrug resistance in cancer therapy and studying P-glycoprotein's role in drug disposition. -
P-glycoprotein Inhibitor
Dofequidar fumarate is a potent P-glycoprotein (P-gp) inhibitor that also targets multidrug resistance-associated protein-1 (MDR-1). This quinoline compound effectively reverses multidrug resistance in tumor cells by competitively inhibiting ABCB1/P-gp and ABCC1/MRP-1. By blocking the efflux of chemotherapeutic agents, Dofequidar fumarate increases drug concentration within cancer cells, thereby enhancing the efficacy of chemotherapy. Its application is particularly relevant in cancer research focused on overcoming drug resistance. -
P-glycoprotein Inhibitor
Reversin 121 is a potent P-glycoprotein inhibitor that enhances the ATPase activity of the MDR1 gene product. By reversing P-glycoprotein-mediated multidrug resistance, it plays a critical role in overcoming drug resistance in cancer therapies. This compound is valuable for research applications focused on enhancing the efficacy of anticancer drugs in resistant cancer cell lines. -
P-gp Inhibitor/Potassium Channel Activator
GPV0057 is a selective and potent inhibitor of P-glycoprotein (P-gp) and a specific activator of the potassium channel Kir2.1. By competitively binding to the substrate-binding site of P-gp, GPV0057 inhibits ATP-dependent drug efflux, effectively reversing multidrug resistance in tumor cells. Additionally, it stabilizes the open state of Kir2.1, facilitating potassium ion influx. This compound holds potential for research in tumors characterized by high P-gp expression and in conditions such as heart failure and Andersen-Tawil Syndrome that involve Kir2.1 deficiency. -
P-Glycoprotein Inhibitor
Boeravinone B is a dual inhibitor of the NorA efflux pump in Staphylococcus aureus and human P-glycoprotein. This compound exhibits significant anti-biofilm activity and reduces intracellular bacterial invasion. Additionally, Boeravinone B demonstrates potential anti-aging and anti-apoptotic effects under oxidative stress conditions, making it a valuable reagent for research in microbiology and cellular aging pathways. -
P-glycoprotein Inhibitor
PGP-4008 is a selective inhibitor of P-glycoprotein (Pgp), known for its role in multidrug resistance (MDR) in cancer cells. This compound demonstrates significant antitumor activity by enhancing the efficacy of chemotherapeutic agents, particularly Doxorubicin, in murine models characterized by Pgp-mediated resistance. PGP-4008 is valuable for research into overcoming drug resistance in cancer therapy and the modulation of pharmacokinetics in oncology. -
P-glycoprotein Inhibitor
WS-898 is a potent P-glycoprotein inhibitor that effectively reverses paclitaxel resistance in various drug-resistant cancer cell lines, including SW620/Ad300, KB-C2, and HEK293/ABCB1, with IC50 values of 5.0, 3.67, and 3.68 nM, respectively. This compound serves as a valuable tool for research focused on overcoming multidrug resistance in cancer therapeutics. Its ability to inhibit ABCB1 transport activity makes it an important reagent for studies aimed at enhancing the efficacy of chemotherapeutic agents. -
P-gp Inhibitor
YS-370 is a potent and selective inhibitor of P-glycoprotein (P-gp) that exhibits oral bioavailability. It facilitates the P-gp ATPase activity while demonstrating moderate inhibition of CYP3A4. This compound effectively reverses multidrug resistance (MDR) in cell lines such as SW620/AD300 and HEK293T-ABCB1, particularly in conjunction with paclitaxel, leading to enhanced antitumor efficacy. YS-370 is valuable for research focused on overcoming drug resistance in cancer therapy. -
P-gp Inhibitor
Tariquidar dihydrochloride is a potent and selective inhibitor of P-glycoprotein (P-gp), exhibiting a high affinity with a Kd of 5.1 nM. This compound significantly enhances the bioavailability of co-administered drugs by inhibiting P-gp-mediated drug efflux. It is widely used in research to investigate the roles of P-gp in pharmacokinetics, drug-drug interactions, and multidrug resistance in cancer therapies. -
P-gp Inhibitor
OY-101 is a potent and orally active inhibitor of P-glycoprotein (P-gp). This compound demonstrates the ability to sensitize drug-resistant tumors, effectively reversing multidrug resistance in cancer cells. With improvements in water solubility, cytotoxicity, and reversal activity compared to Tetrandrine, OY-101 represents a valuable tool in cancer research and development of therapeutic strategies for overcoming drug resistance. -
ABCB1 Inhibitor
Tariquidar dimesylate is a potent ABCB1 inhibitor targeting P-glycoprotein (P-gp). By binding to P-glycoprotein, it effectively increases the concentration of therapeutic agents within the brain, inhibiting their active transport out of cerebral tissue. This compound is invaluable for investigating blood-brain barrier permeability and understanding mechanisms of multidrug resistance in cancer and neurological research. -
P-glycoprotein Inhibitor
Encequidar mesylate hydrochloride is a selective inhibitor of P-glycoprotein (MDR1), which plays a crucial role in drug resistance. This compound enhances the anti-tumor efficacy of Paclitaxel in various mouse tumor models, making it valuable for cancer research. Encequidar mesylate hydrochloride is primarily utilized to study drug interactions and to evaluate therapeutic strategies aimed at overcoming multidrug resistance in cancer treatment. -
P-gp Inhibitor
P-gp Inhibitor 17 is a selective inhibitor of P-glycoprotein (P-gp), directly targeting its transmembrane domain to modulate its activity. This compound is particularly useful for investigating P-gp-mediated multidrug resistance in cancer cells, providing insights into therapeutic strategies for overcoming resistance in oncology research. Its role in enhancing drug bioavailability and efficacy makes it a valuable tool for studying tumor cell behavior and treatment response. -
P-gp Inhibitor
P-gp Inhibitor 13 specifically targets P-glycoprotein (P-gp), functioning as an inhibitor to reverse P-glycoprotein-mediated drug resistance. This compound has demonstrated effectiveness in overcoming paclitaxel resistance in A2780/T cells, making it a valuable tool in cancer research. Its applications extend to the study of advanced acute myeloid leukemia, providing insights into therapeutic strategies for overcoming resistance in this malignancy. -
P-gp Inhibitor
P-gp inhibitor 14 is a potent inhibitor of P-glycoprotein (P-gp), effectively reversing P-gp-mediated multidrug resistance with an EC50 value of 48.74 nM. This compound demonstrates a weak inhibitory effect on CYP3A4 activity, making it a useful agent for enhancing the efficacy of chemotherapeutics in resistant cancer cells. Its primary applications include studies on drug transport mechanisms and overcoming resistance in multidrug-resistant tumors.
