-
Serotonin Reuptake Inhibitor
DA-8031 is a selective serotonin reuptake inhibitor (SSRI) with oral bioavailability. It demonstrates the ability to modulate serotonin levels, making it a valuable compound for studying conditions related to serotonin dysregulation, particularly premature ejaculation (PE). This compound serves as an important tool for research into therapeutic interventions for PE and related disorders. -
Serotonin Reuptake Inhibitor
Lubazodone is a selective serotonin reuptake inhibitor (SSRI) that primarily targets the serotonin transporter. It exhibits significant antidepressant activity and is utilized in the investigation of various depressive disorders. Research applications include exploring its effects on mood regulation and neurochemical pathways associated with depression. -
H+, K+-ATPase Inhibitor
Esomeprazole magnesium, a potent H+, K+-ATPase inhibitor, is utilized in research related to upper intestinal disorders and gastroesophageal reflux disease. Its primary mechanism involves the inhibition of proton pumps, leading to decreased gastric acid secretion. Additionally, Esomeprazole magnesium exhibits properties as an exosome inhibitor by blocking exosome release through the inhibition of vacuolar H+-ATPases, making it valuable for studies on cellular communication and disease progression. -
Sodium Channel Inhibitor
Mepivacaine hydrochloride is a sodium channel inhibitor that selectively binds to voltage-gated sodium ion channels in neuronal cell membranes. By inhibiting sodium influx and membrane depolarization, it provides significant local anesthetic effects. This compound is widely used in research applications related to nerve conduction studies and pain management investigations. -
SERCA Inhibitor
2,5-Di-tert-butylhydroquinone is a potent inhibitor of Sarco/endoplasmic reticulum Ca2+ ATPase (SERCA), demonstrating an IC50 of 400 nM. This compound disrupts the gating function of Glu309, thereby preventing calcium ions from accessing their binding site. Additionally, 2,5-Di-tert-butylhydroquinone influences the activity of key enzymes such as 5-lipoxygenase and COX-2, with IC50 values of 1.8 μM and 14.1 μM, respectively. It is utilized in research focused on cellular calcium regulation and inflammatory processes. -
Bacterial Inhibitor
Methyl Paraben is a bacterial inhibitor primarily used as a preservative in various applications due to its stability and non-volatility. It has been shown to enhance histamine release and modulate cellular immune responses, in addition to blocking sodium channels. Its properties make it valuable for studies exploring microbial inhibition and the mechanisms of ischemia-reperfusion injury. -
TASK-1 Inhibitor
Doxapram hydrochloride hydrate is a TASK-1 inhibitor that enhances respiratory function by stimulating the brain's respiratory centers and peripheral chemoreceptors. This compound effectively increases both the rate and depth of breathing, while demonstrating inhibitory effects on TASK-1, TASK-3, and their heterodimeric channels with EC50 values of 410 nM, 37 μM, and 9 μM, respectively. Additionally, it inhibits Ca²⁺-activated and Ca²⁺-independent potassium currents in type I cells of the carotid body, with IC50 values of approximately 13 μM and 20 μM, respectively. Doxapram hydrochloride hydrate serves as a useful reagent for research on respiratory depression conditions, including post-anesthesia recovery, chronic obstructive pulmonary disease, and apnea of prematurity. -
Calcium Channel Inhibitor
Ethosuximide is a calcium channel inhibitor primarily targeting T-type calcium channels, specifically blocking low voltage-activated currents. This compound is extensively used in research for its anti-epileptic properties as well as its potential therapeutic effects in various neurodegenerative disease models. Ethosuximide facilitates the study of calcium signaling pathways and their involvement in neuronal excitability and degeneration. -
Dopamine Receptor Inhibitor
Fluphenazine dihydrochloride is a potent dopamine receptor antagonist primarily targeting dopamine D2 receptors in the mesolimbic, nigrostriatal, and tuberoinfundibular pathways. This phenothiazine derivative also exhibits the ability to inhibit neuronal voltage-gated sodium channels. Its key biological activities include the suppression of Methylphenidate-induced stereotyped behaviors and climbing in murine models. Fluphenazine dihydrochloride is widely utilized in research related to psychosis, diabetic peripheral neuropathy, and may also have implications for the inhibition of SARS-CoV-2. -
Sodium Channel Inhibitor
Oxybuprocaine hydrochloride is a sodium channel inhibitor that reversibly blocks sodium channels, effectively preventing the propagation of painful nerve impulses in tissues such as the cornea, conjunctiva, and sclera. This compound is primarily utilized in ophthalmology and otolaryngology for its anesthetic properties, providing localized pain relief during various medical procedures. Its ability to inhibit nerve signal transmission makes it valuable for both diagnostic and therapeutic applications in ocular and ear, nose, and throat treatments. -
Sodium Channel Inhibitor
Propafenone hydrochloride is a sodium channel inhibitor primarily used as an anti-arrhythmic agent. It effectively treats conditions related to rapid heartbeats, including atrial and ventricular arrhythmias. This compound is useful in research applications focused on cardiac rhythm disturbances and the pharmacological modulation of ion channels. -
Sodium Channel Inhibitor
Triamterene is a sodium channel inhibitor that selectively blocks epithelial Na+ channels (ENaC) in a voltage-dependent manner. It exhibits mild diuretic properties and is utilized in the management of conditions related to fluid retention. Additionally, Triamterene serves as an inhibitor of the TGR5 receptor, contributing to its diverse biological effects and applications in research related to renal and metabolic processes. -
Sodium Channel Inhibitor
Ropivacaine mesylate acts primarily as a sodium channel inhibitor, serving as a long-acting amide local anesthetic. It effectively blocks impulse conduction by reversibly inhibiting sodium ion influx in nerve fibers, making it suitable for procedures requiring spinal block anesthesia. Additionally, Ropivacaine has been identified as an inhibitor of the K2P potassium channel TREK-1, exhibiting an IC50 value of 402.7 μM in COS-7 cell membranes. This compound is relevant for research into pain management and neuronal activity modulation. -
Sodium Channel Inhibitor
Mepivacaine is an amide-type local anesthetic that functions as a sodium channel inhibitor. By binding to specific voltage-gated sodium ion channels in neuronal cell membranes, Mepivacaine effectively inhibits sodium influx and membrane depolarization. This agent is primarily utilized in various research applications within the fields of pain management and anesthesia. -
Potassium Channel Inhibitor
Cloperastine hydrochloride is a potassium channel inhibitor primarily targeting hERG K+ currents. It demonstrates concentration-dependent inhibition, with an IC50 value of 27 nM. This reagent is employed in research applications focused on cardiac ion channel function and drug interactions, providing valuable insights into cardiovascular safety and pharmacology. -
Proton Pump Inhibitor
Ilaprazole sodium is a potent proton pump inhibitor that irreversibly targets H+/K+-ATPase, demonstrating a dose-dependent inhibition with an IC50 of 6 μM in rabbit parietal cell assays. This compound is primarily utilized in research focused on gastric ulcers, providing insights into gastric acid secretion regulation. Additionally, Ilaprazole sodium acts as an effective inhibitor of TOPK (T-lymphokine-activated killer cell-originated protein kinase), facilitating studies related to immune responses and cancer therapeutics. -
VMAT2 Inhibitor
Valbenazine tosylate is a selective inhibitor of the vesicular monoamine transporter 2 (VMAT2), exhibiting a Ki value in the range of 110-190 nM. It is primarily employed in research related to neuropharmacology and the treatment of movement disorders, such as tardive dyskinesia. By inhibiting VMAT2, Valbenazine tosylate modulates neurotransmitter release, making it a valuable tool for studying dopaminergic signaling and associated pathologies. -
Sodium Channel Inhibitor
Riluzole hydrochloride is a sodium channel inhibitor that exhibits anticonvulsant properties. It functions primarily as a use-dependent Na+ channel blocker and also has the capability to inhibit GABA uptake, with an IC50 of 43 μM. This compound is commonly utilized in neurological research applications, particularly in studies focused on epilepsy and neuroprotection. -
Sodium Channel Inhibitor
Ropivacaine hydrochloride is a potent sodium channel inhibitor that effectively disrupts impulse conduction by reversibly blocking sodium ion influx in nerve fibers. Additionally, it inhibits the K2P TREK-1 potassium channel with an IC50 of 402.7 μM in COS-7 cell membranes. This compound is primarily applied in the management of neuropathic pain in various in vivo research contexts. -
Potassium Channel Inhibitor
Cloperastine fendizoate is a potent inhibitor of the hERG potassium channels, exhibiting concentration-dependent inhibition with an IC50 value of 27 nM. This compound is primarily utilized in research applications focusing on cardiac ion channel function and related arrhythmia studies. Its effects on potassium currents make it valuable for investigating the electrophysiological properties of cardiac tissues and potential therapeutic interventions. -
Sodium Channel Inhibitor
Propoxycaine hydrochloride is a sodium channel inhibitor that disrupts voltage-gated sodium channel activity, leading to a reduction in ionic flux essential for the initiation and propagation of action potentials. This compound is primarily utilized in research to investigate sensory nerve function and analgesic mechanisms, resulting in local anesthetic effects characterized by a loss of sensation. -
Potassium Channel Inhibitor
Tetraethylammonium chloride is a non-selective inhibitor of potassium channels, effectively blocking their function. This compound is recognized as a substrate for organic cation transporter 1 (OCTN1), which may be relevant in transport-related studies. Additionally, tetraethylammonium chloride exhibits potential antitumor properties, making it a valuable tool in cancer research and investigations into ion channel dynamics. -
FTO Inhibitor
Meclofenamic acid is a highly selective inhibitor of the fat mass and obesity-associated (FTO) enzyme, which plays a crucial role in the regulation of m(6)A RNA methylation. By competing with FTO for binding to m(6)A-containing nucleic acids, it modulates RNA metabolism and influences cellular processes related to metabolism and obesity. Additionally, Meclofenamic acid exhibits non-selective blockade of gap junctions and inhibits the potassium channels hKv2.1 and hKv1.1, with IC50 values of 56.0 µM and 155.9 µM, respectively. This compound is valuable for research applications focused on obesity, metabolic regulation, and ion channel physiology. -
T-channels Inhibitor
1-Octanol is a saturated fatty alcohol that selectively inhibits T-type calcium channels, demonstrating an IC50 of 4 μM for native T-currents. This compound serves as a valuable tool in pharmacological research aimed at understanding calcium signaling pathways. Additionally, its properties as a biofuel with diesel-like characteristics make it an interesting candidate for energy applications. -
Nav1.7 Inhibitor
Nav1.7-IN-22 is a selective inhibitor of the voltage-gated sodium channel Nav1.7. By blocking the activity of Nav1.7, this compound effectively inhibits abnormal electrical signal generation and conduction in sensory neurons. Nav1.7-IN-22 is utilized in research focused on pain mechanisms, providing insights into potential therapeutic applications for pain management. -
Sodium Channel Inhibitor
Decarbamoylsaxitoxin is a potent sodium channel inhibitor that selectively blocks the influx of sodium ions in excitable tissues, such as nerve and skeletal muscle cells, thus preventing action potential generation. As a hydrolysis product of saxitoxin, Decarbamoylsaxitoxin exhibits similar neurotoxic effects, including the ability to inhibit veratridine- and ouabain-induced neuroblastoma cell swelling and lysis. This reagent is valuable for research involving mechanisms of paralytic shellfish poisoning and sodium channel pharmacology. -
EBP Inhibitor
EBP-IN-1 is a selective inhibitor of emopamil binding protein (EBP) that effectively crosses the blood-brain barrier. This compound demonstrates an IC50 of 8.2 μM against human ERG potassium channels in CHO cells, leading to the inhibition of EBP's sterol isomerase activity and subsequent accumulation of Zymostenol. EBP-IN-1 has been shown to promote oligodendrocyte differentiation in human cortical organoids, making it a valuable tool for research into multiple sclerosis and related neurological disorders. -
AMPAR Inhibitor.
D15 is an AMPA receptor (AMPAR) endocytosis inhibitor derived from a 15 amino acid segment of dynamin. It inhibits the interaction of dynamin with amphiphysin 1 and 2, leading to a significant increase in AMPAR excitatory postsynaptic potential (EPSC) amplitude in medium spiny neurons (MSNs) within Sapap3 knockout mice. This peptide has valuable applications in the investigation of neuropsychiatric disorders and related signaling pathways. -
AMPA Receptor Inhibitor
AMPA-IN-1 is a potent inhibitor of the AMPA receptor, which is critical for fast excitatory synaptic transmission and synaptic plasticity in the brain. By modulating AMPA receptor activity, AMPA-IN-1 demonstrates potential for research into various central nervous system disorders, including epilepsy. This compound may provide valuable insights into therapeutic strategies targeting excitatory neurotransmission. -
AMPA Inhibitor
AMPA-IN-2 is a potent orally active inhibitor of alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptors, efficiently crossing the blood-brain barrier. This compound demonstrates significant anti-epileptic effects by reducing neuronal excitability and attenuating glutamatergic transmission. AMPA-IN-2 is effective in the pentylenetetrazol model of epilepsy, making it a promising candidate for research in the field of epilepsy and related neuronal excitability disorders. -
Transporter Inhibitor
Pseudoisocyanine iodide, also known as 1,1'-Diethyl-2,2'-cyanine iodide, functions as an inhibitor of organic cation transporters (OCT1, OCT2, OCT3) and the plasma membrane monoamine transporter (PMAT). This compound exhibits antidepressant activity, making it valuable for research in mental health and neuropharmacology. Its ability to modulate transporter function positions it as a useful tool for studying mechanisms of neurotransmitter regulation and potential therapeutic interventions in mood disorders. -
NET Inhibitor
Nisoxetine is a potent and selective inhibitor of the norepinephrine transporter (NET) with a Kd of 0.76 nM. This compound exhibits antidepressant properties and functions as a local anesthetic, in addition to blocking voltage-gated sodium channels. Its mechanisms make it valuable for research in neuropharmacology and the investigation of depression and pain pathways. -
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 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. -
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. -
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. -
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. -
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. -
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. -
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.

