Catalog No.
Product Name
Application
Product Information
Citations
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FFNs
FFN511 is a potent fluorescent false neurotransmitter targeting the vesicular monoamine transporter 2 (VMAT2). With an IC50 of 1 µM, FFN511 effectively inhibits serotonin binding to VMAT2-containing membranes. This compound enables direct imaging of neurotransmitter release dynamics during exocytosis and is particularly useful for labeling dopamine terminals in live cortical-striatal acute slices, facilitating in-depth studies of synaptic function and neurotransmission. -
Monoamine Transporter Inhibitor
(+)-Tetrabenazine is a reversible inhibitor of the vesicular monoamine transporter 2 (VMAT-2). It exhibits a potency that is 10-fold greater for VMAT-2 than for VMAT-1, effectively restricting monoamine transport. This compound is primarily utilized in research focused on neurochemical pathways and the treatment of movement disorders, such as Huntington's disease and tardive dyskinesia, by regulating dopamine levels in the synaptic cleft. -
VMAT2 Substrate
FFN200 dihydrochloride is a fluorescent substrate targeting the vesicular monoamine transporter 2 (VMAT2). This compound enables the selective tracing of monoamine exocytosis in neuronal cell cultures and brain tissue, making it a valuable tool for neuropharmacological studies. With fluorescence excitation and emission maxima at 352 nm and 451 nm, respectively, FFN200 dihydrochloride is well-suited for applications requiring high sensitivity and specificity in monitoring neurotransmitter release. -
TBZ Metabolite
(R,S,S)-Dihydrotetrabenazine is a secondary alcohol metabolite derived from Tetrabenazine, functioning primarily as a poor inhibitor of the vesicular monoamine transporter 2 (VMAT2) with a Ki value of 690 nM. This compound is utilized in neuropharmacological studies to investigate the modulation of monoamine transporters and their role in diseases such as Parkinson's and Huntington's. Its unique isomeric structure allows for in-depth research into the pharmacokinetics and pharmacodynamics of related compounds. -
VMAT2 Inhibitor
Dihydrotetrabenazine (DHTBZ) is a selective inhibitor of the vesicular monoamine transporter 2 (VMAT2). By decreasing the monoamine content in presynaptic neurons, it plays a crucial role in the study of movement disorders. DHTBZ is essential for investigating the mechanisms underlying neurotransmitter regulation and offers potential insights into therapeutic strategies for neurological diseases. -
Drug Derivative
4-Ethyl-N,N-Dmc hydrochloride is a drug derivative acting as a non-selective substrate for monoamine transporters, which enhances the release of neurotransmitters. This compound is primarily utilized in research focused on the pharmacological effects of amphetamines and related substances. Its structural modifications offer insights into the development of novel psychoactive compounds and their interactions within the central nervous system. -
VMAT2 Inhibitor
(-)-Tetrabenazine is a specific inhibitor of the vesicular monoamine transporter 2 (VMAT2). This compound exhibits notable biological activity in the modulation of monoamine neurotransmitter levels, making it valuable for research in neuropharmacology and the study of movement disorders. Its role as a VMAT2 inhibitor can aid in the investigation of drug development for conditions such as Huntington's disease and other neurodegenerative disorders. -
Deuterated (+)-Tetrabenazine
(+)-Tetrabenazine-d6 is a deuterated form of the reversible inhibitor (+)-Tetrabenazine, which targets the vesicular monoamine transporter 2 (VMAT-2). This compound is utilized in research to investigate neurochemical processes and the role of monoamines in neurological disorders. Its isotopic labeling facilitates advanced metabolic studies and pharmacokinetic evaluations in biological systems. -
VMAT2 Inhibitor
Tetrabenazine mesylate is a potent reversible inhibitor of the vesicular monoamine transporter VMAT2, with a Kd value of 1.34 nM. This compound is primarily used in research focused on hyperactive movement disorders, including Huntington's disease, due to its ability to modulate monoamine neurotransmitter release. Tetrabenazine mesylate serves as a valuable tool for studying the underlying mechanisms of these neurological conditions and evaluating potential therapeutic approaches. -
VMAT2 Inhibitor
Tetrabenazine Metabolite is a potent vesicular monoamine transporter 2 (VMAT2) inhibitor, exhibiting high affinity with a Ki of 13.4 nM. This active metabolite plays a crucial role in the modulation of monoamine neurotransmitter levels and is primarily investigated for its therapeutic potential in chorea associated with Huntington’s disease and other hyperkinetic disorders. Its mechanism of action supports ongoing research in neurological disease management and treatment strategies. -
VMAT2 Inhibitor
VMAT2-IN-2 tosylate is a potent inhibitor of the vesicular monoamine transporter 2 (VMAT2). This compound is essential for investigating the pathophysiology of conditions such as tardive dyskinesia, where dysregulation of neurotransmitter storage and release plays a critical role. VMAT2-IN-2 tosylate may provide valuable insights into therapeutic strategies and the development of treatment options for related neurological disorders. -
Metabolite of Tetrabenazine
Trans (2,3)-Dihydrotetrabenazine is a metabolite of Tetrabenazine that primarily targets the vesicular monoamine transporter 2 (VMAT2). It exhibits significant inhibitory activity on VMAT2, contributing to altered monoamine storage and release. This compound is valuable for research applications in neuropharmacology and the study of movement disorders, providing insights into the modulation of neurotransmitter systems. -
Stable Isotope
Tetrabenazine-d7 is a deuterium-labeled derivative of Tetrabenazine, a reversible inhibitor of the vesicular monoamine transporter VMAT2, demonstrating a Kd value of 1.34 nM. This compound is essential in biochemical research focused on hyperkinetic movement disorders, including Huntington's disease. The stable isotope labeling allows for enhanced tracking and analysis in metabolic studies and pharmacokinetic evaluations. -
DAT/NET/SERT Agonist
2-(tert-Butylamino)-1-phenylpropan-1-one hydrochloride is a non-selective agonist of monoamine transporters, specifically targeting dopamine (DAT), norepinephrine (NET), and serotonin (SERT). This compound exhibits significant activity in modulating monoamine neurotransmission, making it a valuable tool for investigating the biochemistry underlying depressive disorders. It serves as a useful reagent in pharmacological studies aimed at understanding the mechanisms of mood regulation and potential therapeutic approaches. -
Monoamine Transporter Inhibitor
13-Hydroxyisobakuchiol is a selective inhibitor of monoamine transporters, primarily targeting the dopamine transporter (DAT) and norepinephrine transporter (NET) with IC50 values of 0.58 μM and 0.69 μM, respectively. In contrast, it exhibits significantly lower affinity for the serotonin transporter (SERT), with an IC50 of 312.02 μM. This compound is valuable for research applications related to neurodegenerative diseases, including Parkinson's disease, and mood disorders such as depression. -
Monoamine Transporter Inhibitor
Cendifensine is a monoamine transporter inhibitor that targets the serotonin transporter (SERT), norepinephrine transporter (NET), and dopamine transporter (DAT). It is known for its ability to inhibit the reuptake of these key neurotransmitters, thus enhancing their availability in the synaptic cleft. This compound is primarily utilized in research to study the mechanisms of mood disorders, depression, and other neurological conditions, making it a valuable tool for neuroscientific investigations. -
VMAT2 Inhibitor
(2S,3S,11bR)-Dihydrotetrabenazine is a selective inhibitor of the vesicular monoamine transporter 2 (VMAT2), exhibiting a Ki value of 593 nM. This compound disrupts the vesicular transport of monoamine neurotransmitters, including dopamine and serotonin, leading to decreased synaptic release of these neurotransmitters. (2S,3S,11bR)-Dihydrotetrabenazine is valuable for research into Huntington's chorea and other hyperkinetic disorders, providing insights into potential therapeutic strategies. -
Monoamine Transporter
4-Methyl-α-ethyltryptamine functions primarily as a monoamine transporter modulator. This compound is known to influence the release and re-uptake of monoamines within the brain, making it potentially valuable for research into neurochemical pathways. Its structural similarities to α-Ethyltryptamine suggest its utility in studying the effects of tryptamine derivatives on neurotransmitter dynamics and behavior. -
VMAT2 Inhibitor
VMAT2-IN-4 is a selective inhibitor of the vesicular monoamine transporter-2 (VMAT2), demonstrating an affinity with a Ki value of 560 nM for [3H]-DTBZ binding and a more potent inhibition of [3H]-DA uptake into vesicles at a Ki of 45 nM. This compound effectively disrupts monoamine neurotransmitter packaging within vesicles, making it a valuable tool for investigating the mechanisms underlying methamphetamine addiction. VMAT2-IN-4 supports research into the modulation of dopaminergic signaling and its implications in addiction studies. -
FFNs
FFN511 hydrochloride is a potent fluorescent false neurotransmitter (FFN) that selectively targets the vesicular monoamine transporter 2 (VMAT2). With an IC50 of 1 µM, it effectively inhibits serotonin binding to VMAT2-containing membranes. This compound enables real-time imaging of neurotransmitter release dynamics during exocytosis and is particularly useful for labeling dopamine terminals in live cortical-striatal acute slices, making it a valuable tool for studying synaptic transmission and neuropharmacology. -
VMAT2 Inhibitor
GZ-11608 is a potent and selective inhibitor of the vesicular monoamine transporter-2 (VMAT2) with a high affinity (Ki = 25 nM). This compound effectively reduces methamphetamine-induced dopamine release from isolated synaptic vesicles of dopaminergic neurons. Furthermore, GZ-11608 demonstrates rapid penetration into the brain and is characterized by an absence of neurotoxicity. It is a valuable tool for studying methamphetamine use disorder in therapeutic research. -
Monoamine Transporter
3-Bromoamphetamine hydrochloride is a para-substituted amphetamine that functions as a monoamine releasing agent, primarily targeting the monoamine transporters. This compound has been shown to facilitate the release of neurotransmitters such as serotonin, dopamine, and norepinephrine, making it valuable in studies of neuropharmacology and behavior. Its applications in research include investigations of mood disorders, stimulant effects, and the underlying mechanisms of psychoactive substances. -
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.
