Catalog No.
Product Name
Application
Product Information
Citations
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MCT4 Inhibitor
VB124 is a potent and selective inhibitor of monocarboxylate transporter 4 (MCT4), demonstrating significant activity with IC50 values of 8.6 nM and 19 nM for lactate import and export in MDA-MB-231 cells, respectively. VB124 exhibits high selectivity for MCT4, distinguishing it from MCT1. This compound is valuable for research in areas such as cardiac hypertrophy, heart failure, and metabolic studies. -
MCT1/MCT4 Dual Inhibitor
Syrosingopine is a dual inhibitor of lactate transporters MCT1 and MCT4, effectively reducing glycolytic metabolism in cancer cells when combined with metformin. This compound has been shown to induce synthetic lethality, making it a valuable tool for cancer research. Additionally, Syrosingopine exhibits anti-hypertensive properties by depleting peripheral norepinephrine stores, presenting further avenues for cardiovascular studies. -
MCT4 Inhibitor
AZD0095 is a selective, orally bioavailable inhibitor of monocarboxylate transporter 4 (MCT4), characterized by an IC50 of 1.3 nM. This compound demonstrates significant antitumor activity by effectively inhibiting tumor growth in NCI-H358 xenograft models, particularly in combination with Cediranib. AZD0095 serves as a valuable tool for research into metabolic modulation and therapeutic strategies in cancer biology. -
MCT4 Inhibitor
MSC-4381 is a selective inhibitor of monocarboxylate transporter 4 (MCT4/SLC16A3), exhibiting an IC50 of 77 nM and a Ki of 11 nM. This compound effectively inhibits lactate efflux and decreases cellular viability in cells with high MCT4 expression. MSC-4381 serves as a valuable tool for research involving MCT4 transporter inhibition and features a reactive alkyne group, enabling copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules. -
MCT Inhibitor
MCT-IN-1 is a potent inhibitor of monocarboxylate transporters (MCT1 and MCT4), exhibiting IC50 values of 9 nM and 14 nM, respectively. This compound is particularly relevant for research into solid tumors, offering valuable insights into metabolic modulation and therapeutic strategies targeting tumor microenvironments. MCT-IN-1 serves as a crucial tool for investigating the role of lactate transport in cancer cell proliferation and survival. -
PepT1/MCT1 Inhibitor
N-Acetyl-R-leucine is an N-substituted chiral amino acid that functions as an inhibitor of the peptides transporter PepT1 and the monocarboxylate transporter MCT1, with IC50 values of 0.74 mM and 11 mM, respectively. This compound is valuable for investigating transporter activity and can be utilized in LysoTracker signaling studies, contributing to research on cellular metabolism and related pathways. -
MCT1 Inhibitor
MCT1-IN-2 is a potent inhibitor of monocarboxylate transporter 1 (MCT1), which plays a key role in cellular metabolism by facilitating the transport of lactate and other monocarboxylates. This compound has demonstrated significant anti-cancer activity, making it a valuable tool for research in cancer metabolism and therapeutic development. MCT1-IN-2 is suitable for studies investigating the role of MCT1 in tumor growth and progression, as well as potential combination therapies targeting metabolic pathways in cancer cells. -
MCT1 Inhibitor
MCT1-IN-3 is a potent inhibitor of the monocarboxylate transporter 1 (MCT1), exhibiting an IC50 value of 81.0 nM. Additionally, this compound shows significant inhibitory activity against the multidrug transporter ABCB1. MCT1-IN-3 is valuable for research applications focused on cancer, particularly in elucidating the role of MCT1 in tumor metabolism and drug resistance. -
MCT Inhibitor
AR-C141990 hydrochloride is a selective inhibitor of monocarboxylate transporters (MCTs), specifically demonstrating pKi values of 7.6 and 6.6 for MCT-1 and MCT-2, respectively. This compound exhibits immunosuppressive properties and is utilized in research concerning graft versus host disease and metabolic regulation. Its ability to modulate lactate transport makes it a valuable tool for studying the role of MCTs in various biological processes. -
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. -
Calcium Channel Blocker
Suloctidil is an orally active calcium channel blocker that primarily targets vasoconstriction pathways. It effectively antagonizes vasoconstriction induced by norepinephrine, angiotensin, and serotonin, while also inhibiting platelet function and exhibiting neuroprotective effects. Additionally, Suloctidil demonstrates antifungal activity against Candida albicans, influencing biofilm formation and virulence. This compound is applicable in research focused on vasospasm relief, antithrombosis, and treatment of superficial candidiasis. -
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. -
Na+/K+ ATPase Control
Ro18-5362 is a proagent of Ro18-5364 that targets Na+/K+ ATPase. While it exhibits limited activity on (H++K+)-ATPase at concentrations up to 0.1 mM, it serves as a useful tool for understanding ATPase mechanisms and probing related physiological processes. This compound is valuable in research focusing on ion transport regulation and cellular homeostasis. -
KATP Opener
Iptakalim hydrochloride is a selective ATP-sensitive potassium channel (KATP) opener that exhibits significant lipophilicity. In addition to its primary mechanism, it also acts as an antagonist of α4β2-containing nicotinic acetylcholine receptors (nAChRs). This dual activity positions Iptakalim hydrochloride as a valuable tool for research in cardiovascular physiology and neuropharmacology, providing insights into potassium channel regulation and cholinergic signaling. -
KCC2 Antagonist
ML077 is a selective antagonist of the potassium-chloride co-transporter 2 (KCC2), with an IC50 of 537 nM for KCC2, while exhibiting minimal activity on KCC1 (IC50 > 50 μM). By inhibiting the chloride ion excretion function of KCC2, ML077 increases intracellular chloride concentrations, resulting in enhanced depolarization through chloride channels. This compound has demonstrated the ability to promote glucose-stimulated insulin secretion (GSIS) independent of KATP channels and is valuable for studying the physiological processes related to pain, epilepsy, and insulin secretion. -
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.
