Catalog No.
Product Name
Application
Product Information
Citations
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Autophagy Inducer
Diazoxide is an ATP-sensitive potassium channel activator that induces autophagy through modulation of cellular ion balance. This compound demonstrates potential therapeutic effects in conditions related to hyperinsulinism. It is commonly utilized in research applications focusing on autophagy pathways and metabolic regulation. -
Kir2.1 Agonist
Tetramisole hydrochloride is a selective inward rectifier potassium channel agonist that primarily targets the Kir2.1 subunit with an EC50 of approximately 30 μM. This compound plays a crucial role in promoting Kir2.1 channel functioning, hyperpolarizing the resting potential, and shortening action potential duration. Additionally, it exhibits effects on intracellular calcium regulation while influencing PKA signaling, contributing to its anti-arrhythmic and anti-myocardial remodeling properties. Tetramisole hydrochloride is valuable for investigations in cardiac electrophysiology, as well as studies focused on myocardial ischemia and heart failure. -
KATP Inhibitor
Tolbutamide is an orally active KATP inhibitor that primarily targets ATP-sensitive potassium channels. It is known to inhibit cell proliferation and stimulate the exocytosis of glucagon, while also reducing fetal lethality in murine models. This compound is utilized in diabetes research to explore mechanisms of insulin secretion and glucose metabolism. -
Proton Pump Inhibitor
Omeprazole sodium is a proton pump inhibitor (PPI) that effectively reduces gastric acid secretion, making it useful in treating acid-related gastrointestinal disorders. In addition to its primary role, omeprazole sodium competitively inhibits CYP2C19 with a Ki value ranging from 2 to 6 μM, which may influence drug metabolism. This compound also displays antibacterial activity against both Gram-positive and Gram-negative bacteria, and it serves as a potent inhibitor of neutral sphingomyelinase (N-SMase), impacting exosome production. Its diverse biological activities make it a valuable tool for research in pharmacology and microbiology. -
Calcium Channel Blocker
Dotarizine is a selective calcium channel blocker that functions by inhibiting Ca2+ influx. This compound demonstrates significant antimigraine activity through its modulation of calcium signaling pathways. Additionally, Dotarizine reduces the release of lactate dehydrogenase and exhibits the capacity to block 5-HT receptors, making it a valuable tool for research in neural signaling and migraine pathophysiology. -
Monoamine Transporter Modulator
6-APDB is a monoamine transporter modulator that selectively influences human monoamine transporters while acting as a partial agonist at 5-HT2 family receptors. It demonstrates potent inhibition of norepinephrine and serotonin reuptake, with IC50 values of 0.56 μM for norepinephrine transporters (NET) and 2.3 μM for serotonin transporters (SERT). Additionally, 6-APDB mediates the release of multiple monoamine neurotransmitters, exhibiting a dose-dependent, biphasic locomotor effect in mice. This compound also has potential empathogenic properties along with behavioral effects relevant to research on monoamine signaling and neuropsychopharmacology, with no significant cytotoxicity observed at high concentrations. -
Calcium Channel Blocker
Levemopamil hydrochloride is a calcium channel blocker that effectively penetrates the blood-brain barrier and acts as a 5-HT2 antagonist. This compound exhibits key biological activity in modulating calcium influx, making it valuable for research related to temporary occlusion and various neurological diseases. It serves as a useful tool for studying the effects of calcium channel modulation on neuronal function and pathophysiology. -
Calcium Channel Blocker
Levemopamil is a calcium channel blocker known for its ability to antagonize 5-HT2 receptors. It demonstrates renoprotective properties, particularly in the context of ischemic acute kidney injury. This compound is suitable for research involving ischemic acute renal failure and related nephroprotective studies. -
5-HT(1A/B/D) Receptor Antagonist
GSK-588045 is a potent antagonist of the 5-HT(1A/B/D) receptors, demonstrating a high degree of selectivity for these targets while sparing human ether-a-go-go related gene (hERG) potassium channels. This specificity makes GSK-588045 a valuable tool in the study of neurological disorders, particularly in the context of depression and anxiety research applications. Its unique profile can aid in elucidating the role of serotonin receptors in various neuropsychiatric conditions. -
Calcium Antagonist
Nexopamil is a calcium antagonist that targets Ca2+ channels, as well as 5-HT2, 5-HT1A, 5-HT1C, and dopamine D2 receptors. This compound demonstrates significant vasodilatory and cardioprotective properties, along with the ability to inhibit platelet aggregation. Nexopamil is useful for research focused on conditions such as stable and unstable angina, as well as potentially in studies of peripheral arterial occlusive disease. -
V-ATPase Inhibitor
Bafilomycin D is a specific inhibitor of vacuolar-type ATPase (V-ATPase), blocking proton translocation and disrupting acidic environments within cells. This compound exhibits significant antimicrobial, insecticidal, herbicidal, and cytotoxic activities, making it a valuable tool for biochemical research. It is useful in studies related to cellular metabolism, ion homeostasis, and the investigation of V-ATPase functions across various biological systems. -
Stable Isotope
Anandamide-d8 is a deuterated form of the endocannabinoid Anandamide, primarily known for its interaction with cannabinoid receptors CB1 and CB2. This compound modulates various neuronal and immune functions and can also engage additional receptors, including PPARs, TRPV1, and GPR18/GPR55. Anandamide-d8 exhibits potential anti-fungal and anti-inflammatory properties, making it valuable for research applications in fields such as neurodegenerative diseases, including Alzheimer's disease, and inflammatory conditions like ulcerative colitis. - Sarcosine ethyl ester hydrochloride is a Glycine derivative.
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noradrenalin transporters inhibitor
Desipramine hydrochloride is a tricyclic antidepressant that is a selective inhibitor of noradrenalin transporters (Ki values are 4, 61 and 78720 nM for NET, SERT and DAT transporters respectively).
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Histone Methyltransferase
Lobelane hydrochloride selectively inhibits the vesicular monoamine transporter-2 (VMAT2). This compound demonstrates an affinity for VMAT2 with a K(i) value of 630 nM, while exhibiting low interaction with nicotinic acetylcholine receptors (nAChR). The unique mechanism of action of lobelane hydrochloride makes it a valuable tool for studying neurotransmitter dynamics and offers potential in the development of therapeutic agents aimed at addressing methamphetamine abuse. Its structural analogs may further expand its applications in neuropharmacological research. -
TRPV1 Antagonist
Pellitorine is a natural amide compound that functions as a TRPV1 antagonist, effectively inhibiting pain signal transmission activated by capsaicin. This compound demonstrates significant biological activity by improving cognitive function through the upregulation of BDNF-ERK1/2-CREB and Nrf2-HO-1 pathways. In addition, Pellitorine exhibits anti-inflammatory properties by reducing the release of high mobility group protein B1 (HMGB1) and the expression of RAGE/TLR4. Furthermore, it has antithrombotic effects, mitigates lipid peroxidation, and has exhibited activity against Aedes aegypti mosquito larvae as well as certain cancer types and bacteria, making it a versatile tool in chemical research applications. -
Calcium Channel Blocker
Nitrendipine is a dihydropyridine calcium channel blocker primarily acting on L-type calcium channels. It exhibits significant antihypertensive properties and has been shown to induce apoptosis in various cellular contexts, including neuroblastoma. Additionally, Nitrendipine alleviates withdrawal symptoms associated with alcohol and morphine and reduces right ventricular hypertrophy and pulmonary vascular alterations induced by intermittent hypoxia. Its diverse biological activities make it valuable in research related to cardiovascular health and cancer biology. -
hTRPA1 Antagonist
(E)-Cardamonin is a selective antagonist of the human transient receptor potential ankyrin 1 (hTRPA1) channel, exhibiting an IC50 of 454 nM. This compound is instrumental in research involving nociception and inflammatory pain models, facilitating studies of sensory signaling pathways. Its role in modulating hTRPA1 activity makes it a valuable reagent for exploring channel-related physiological and pathological processes. -
Potassium Channel Inhibitor
Dequalinium Chloride is a selective inhibitor of potassium channels sensitive to Apamin. This cationic, lipophilic compound exhibits mitochondrial toxicity and additionally acts as an antagonist of the α7 nicotinic acetylcholine receptor. Dequalinium Chloride demonstrates broad-spectrum antimicrobial properties, exhibiting both bactericidal and fungicidal activities, making it valuable for research in cellular physiology and microbiology. -
Calcium Channel Blocker
Lercanidipine hydrochloride is a third-generation dihydropyridine calcium channel blocker with a primary mechanism of selectively inhibiting vascular calcium channels. Its potent antihypertensive effects are complemented by reno- and neuro-protective properties, making it valuable for research into cardiovascular and neurological conditions. Additionally, Lercanidipine exhibits anti-oxidant, anti-inflammatory, and anti-apoptotic activities, further supporting its utility in various biomedical applications. -
Proton Pump Inhibitor
Pantoprazole sodium is a potent proton pump inhibitor that specifically targets the H+/K+-ATPase enzyme with an IC50 of 6.8 μM. This substituted benzimidazole effectively reduces gastric acid secretion, demonstrating significant anti-secretory and anti-ulcer activities. Additionally, studies indicate that Pantoprazole sodium can enhance tumor growth delay when used in combination with Doxorubicin, making it a valuable tool in cancer research and gastrointestinal studies. -
Antimicrobial Agent
Zinc Pyrithione is an antimicrobial agent primarily known for its antifungal and antibacterial properties, acting by disrupting membrane transport through the inhibition of proton pumps. Additionally, it functions as a copper ionophore, facilitating the delivery of copper ions into cells. This compound serves as a valuable tool in the study of cuproptosis, providing insights into copper metabolism and its implications in various biological processes. -
Antinociceptive Agent
Citronellyl acetate is a monoterpene compound that serves as an orally active antinociceptive agent. It modulates various targets including TRPV1, TRPM8, ASIC, and glutamate receptors, along with protein kinase pathways PKC and PKA, contributing to its effects on nociception. This compound is valuable for research focused on understanding and managing acute pain mechanisms. -
Mdr1p Inhibitor
P-gp-IN-34 is a potent inhibitor of the Mdr1p pump, targeting multidrug resistance in various biological contexts. It has demonstrated efficacy in inhibiting the yeast-to-hyphal transition in Candida albicans, a critical process in its pathogenicity. This compound is suitable for research applications focused on candidiasis and the mechanisms of antifungal resistance. -
Pma1p-ATPase Inhibitor
ATPase-IN-5 is a potent inhibitor of Pma1p-ATPase, exhibiting an IC50 value of 12.7 μM. This compound is critically important in the study of antifungal mechanisms, providing insights into yeast cell metabolism and enzyme regulation. ATPase-IN-5 offers valuable applications in antifungal research, enabling the exploration of new therapeutic strategies. -
Sodium Channel Inhibitor
Lamotrigine-13C3 is a stable isotope-labeled derivative of Lamotrigine, a highly effective sodium channel inhibitor. This compound selectively targets voltage-gated Na+ channels, leading to stabilization of presynaptic neuronal membranes and a subsequent reduction in glutamate release. Lamotrigine-13C3 is suitable for research applications related to epilepsy, focal seizures, and other neurological disorders. -
Stable Isotope
Omeprazole-d3-1 is a deuterium-labeled form of Omeprazole, a proton pump inhibitor (PPI) primarily targeting acid-related gastrointestinal disorders. This compound exhibits competitive inhibition of CYP2C19, with a Ki ranging from 2 to 6 μM, and has demonstrated antimicrobial effects against both Gram-positive and Gram-negative bacteria. Additionally, Omeprazole acts as a potent inhibitor of neutral sphingomyelinase (N-SMase), impacting exosome production in cell studies. This stable isotope is a valuable tool for pharmacokinetic and metabolic research applications. -
Stable Isotope
Desethyl Amiodarone-d4 hydrochloride is a deuterium-labeled analog of Desethylamiodarone hydrochloride, a significant active metabolite of the antiarrhythmic drug Amiodarone. This compound predominantly arises from the metabolic activity of CYP3A isoenzymes. Desethylamiodarone hydrochloride demonstrates potent inhibition of ATP-sensitive potassium channels, with an IC50 value of 19.1 μM, making it a valuable tool for research in cardiac electrophysiology and drug metabolism studies. -
TRPML Modulator
TRPML modulator 1 is a selective modulator of the TRPML channel, known for its role in promoting autophagy. With an AC50 of less than 2 mM in the TFEB assay, it effectively enhances autophagic flux, making it a valuable tool for research applications focused on cellular degradation processes and lysosomal function. This compound is instrumental in studying the molecular mechanisms underlying autophagy-related diseases. -
Stable Isotope
Diazoxide-d3 is a deuterium-labeled derivative of Diazoxide, an ATP-sensitive potassium channel activator. This compound is primarily utilized in research to investigate insulin regulation and has potential applications in the treatment of hyperinsulinism. Its unique isotopic labeling allows for enhanced tracking and analysis in various biochemical studies. -
Stable Isotope
Omeprazole-d6 is a deuterium-labeled form of Omeprazole, a proton pump inhibitor (PPI) primarily targeting gastric acid secretion. It demonstrates competitive inhibition of CYP2C19 with an inhibition constant (Ki) ranging from 2 to 6 μM, making it a valuable tool in drug metabolism studies. In addition to its role in gastrointestinal health, Omeprazole exhibits antibacterial activity against both Gram-positive and Gram-negative bacteria and serves as a potent inhibitor of neutral sphingomyelinase (N-SMase), thereby impacting exosome production and release. This stable isotope variant is useful for pharmacokinetic studies and tracing in biological research applications. -
ATX Inhibitor/PPARγ Agonist
EL244 is a dual inhibitor of Autotaxin (ATX), with an IC50 of 50 nM, and a selective agonist of PPARγ, exhibiting an IC50 of 1.3 μM. This compound shows low cytotoxicity in human HepG2 cells, with an EC50 of 81.2 μM, and minimal inhibition of the cardiac hERG potassium channel (12% at 25 μM). EL244 effectively reduces pulmonary Lysophosphatidic Acid (LPA) levels, mitigates fibrosis, and enhances respiratory function in vivo, making it a valuable tool for the study of idiopathic pulmonary fibrosis and interstitial lung disease (ILD). -
PPARγ/TRPA1 Receptor Partial Agonist
Neoambrosin is a sesquiterpene lactone that acts as a partial agonist of the PPARγ and TRPA1 receptors. This compound demonstrates potential biological activity related to hypoglycemia, analgesia, anti-inflammatory responses, and anticancer effects. Neoambrosin is suitable for research applications aimed at exploring metabolic disorders and pain management, as well as studying its role in inflammation and cancer therapeutics. -
PPAR Agonist
20-HEPE is a metabolite of eicosapentaenoic acid that functions primarily as a peroxisome proliferator-activated receptor α (PPARα) agonist. At a concentration of 10 μM, it effectively activates PPARα in COS-7 cells that express a luciferase reporter gene. Additionally, 20-HEPE activates the mouse transient receptor potential vanilloid receptor 1 (mTRPV1) in vitro, although it does not exhibit analgesic effects in rat models. This compound has potential applications in the study of metabolic processes and receptor signaling pathways. -
Stable Isotope
Lansoprazole-d4 is a deuterium-labeled derivative of Lansoprazole, a proton pump inhibitor that inhibits gastric acid secretion by targeting the H+/K+ ATPase in the gastric parietal cells. The incorporation of deuterium enhances the stability and can facilitate metabolic studies and pharmacokinetic research applications. This stable isotope-labeled compound is valuable for tracing studies, improving analysis of drug metabolism, and understanding the pharmacodynamics of proton pump inhibitors. -
Stable Isotope
Probenecid-d14 is a deuterated form of Probenecid, which serves as a selective agonist of the transient receptor potential vanilloid 2 (TRPV2) channels. This stable isotope enables precise tracking and quantification in metabolic studies. Additionally, Probenecid-d14 is recognized for its inhibitory effects on pannexin 1 channels, making it a valuable tool for investigating cellular signaling pathways and receptor interactions in various biological research applications. -
H+, K+-ATPase Inhibitor
Esomeprazole hemistrontium is a potent H+, K+-ATPase inhibitor that functions as an effective proton pump inhibitor. It reduces gastric acid secretion by targeting the H+, K+-ATPase enzyme in parietal cells. This compound is particularly valuable for research applications related to symptomatic gastroesophageal reflux disease. -
Potassium-Competitive Acid Blocker
Vonoprazan hydrochloride is a potassium-competitive acid blocker (P-CAB) that inhibits H+,K+-ATPase activity, exhibiting an IC50 of 19 nM at pH 6.5. Its potent antisecretory effects make it a valuable reagent in research related to acid-related conditions, including gastroesophageal reflux disease and peptic ulcer disease. Vonoprazan hydrochloride is also utilized for studies focusing on the eradication of Helicobacter pylori, contributing to advancements in gastrointestinal therapeutics. -
TRPM2 Activator
Adenosine 5′-diphosphoribose sodium is a potent activator of the TRPM2 cation channel, which is permeable to Ca2+. This NAD+ metabolite plays a crucial role in cellular signaling and has been shown to enhance autophagy. It serves as a valuable tool for research investigating calcium signaling pathways and the modulation of autophagy in various biological contexts. -
TRPML1/3 Inhibitor
(rel)-ML-SI3 is a selective inhibitor of TRPML1 and TRPML3, exhibiting IC50 values of 3.1 μM and 28.5 μM, respectively. In contrast, it acts as a potent activator of TRPML2 with an EC50 of 3.3 μM. This compound is valuable for research into the roles of TRPML channels in cellular processes and potential therapeutic interventions in related pathologies. Its specificity for multiple isoforms contributes to its utility in exploring calcium signaling pathways and lysosomal function. -
Antidiabetic Agent
4-Hydroxytolbutamide is a metabolite of Tolbutamide and acts primarily as an antidiabetic agent. It is involved in glucose metabolism by functioning as a potassium channel blocker, influencing insulin secretion from pancreatic beta-cells. This compound is particularly relevant in diabetes research, where it is used to study the pharmacodynamics and pharmacokinetics of sulfonylurea derivatives. Additionally, its metabolism by CYP2C8 and CYP2C9 contributes to understanding drug interactions in antidiabetic therapies. -
L-type Calcium Channel Blocker
Fendiline is an L-type calcium channel blocker that exhibits an IC50 of 17 µM. In addition to its role in cardiovascular modulation, Fendiline acts as a selective inhibitor of K-Ras, with an IC50 of 9.64 μM, effectively preventing K-Ras plasma membrane localization and blocking downstream signaling. This compound has demonstrated potential in inhibiting the proliferation of various cancer cell lines such as pancreatic, colon, lung, and endometrial cancers that express oncogenic mutant K-Ras. Furthermore, Fendiline serves as a STING agonist, showing promise in inhibiting the growth of refractory cold tumors, including MC38, CT26, and B16F10. -
Anti-microbial Agent/Kir3.2 Blocker
3,6-Diaminoacridine dihydrochloride is a potent antimicrobial agent that acts primarily by intercalating into bacterial DNA, disrupting replication and transcription, and leading to bacterial cell lysis. Additionally, it serves as a Kir3.2 potassium channel blocker, making it a valuable tool for investigating neurological conditions such as Down syndrome. Furthermore, due to its ability to penetrate skin layers and accumulate in the cell nucleus, long-term exposure requires careful handling due to potential carcinogenic effects. This reagent is applicable in studies concerning microbial resistance and neurological phenotype exploration. -
Anti-microbial Agent/Kir3.2 Blocker
3,6-Diaminoacridine sulfate functions primarily as an anti-microbial agent and a Kir3.2 potassium channel blocker. This acridine compound exhibits broad-spectrum antibacterial activity by intercalating into bacterial DNA, disrupting replication and transcription, ultimately leading to cell lysis. Additionally, it is utilized in neurological research, particularly in studying the phenotype associated with Down syndrome. Notably, 3,6-Diaminoacridine sulfate exhibits the capability to penetrate the skin's stratum corneum and accumulate in the cell nucleus, with prolonged exposure possibly linked to carcinogenic effects. -
Na+/K+ ATPase Inhibitor
Chamigrenol is an inhibitor of the Na+/K+ ATPase, exhibiting an IC50 value of 15.9 μg/mL. This compound demonstrates significant antibacterial activity against both Gram-positive and Gram-negative bacteria, with the exception of Escherichia coli, showing minimum inhibitory concentration (MIC) values of 50 µg/mL. Chamigrenol is valuable for research in microbiology and the development of novel antimicrobial agents. -
Na+/K+-ATPase Inhibitor
(-)-γ-Cuparenol is a sesquiterpene compound that acts as an inhibitor of Na+/K+-ATPase, with an IC50 value of 23.6 μg/mL in porcine models. It has demonstrated the ability to reduce phytohemagglutinin (PHA)-induced activation of NF-AT and NF-κB in Jurkat cells, indicating potential applications in immunoregulation. Additionally, (-)-γ-Cuparenol exhibits antibacterial activity against certain Gram-positive and some Gram-negative bacteria, as well as weak inhibitory effects on Candida albicans. This compound is relevant for research exploring cardiovascular diseases and bacterial infections. -
TRPV2 Agonist
Probenecid sodium is the sodium salt form of Probenecid, functioning as a selective agonist for the transient receptor potential vanilloid 2 (TRPV2) channel. This compound has been shown to activate TRPV2, contributing to various physiological responses. Additionally, Probenecid sodium inhibits the pannexin 1 channel, making it valuable for studying cellular communication and inflammation processes. Its utility in research extends to investigating the role of TRPV2 in pain sensation and other biological pathways. -
H+, K+-ATPase Inhibitor
Esomeprazole (S-Omeprazole) is a potent H+, K+-ATPase inhibitor that functions as an effective proton pump inhibitor. It reduces gastric acid secretion by specifically inhibiting the H+, K+-ATPase enzyme in parietal cells of the stomach lining. This compound is valuable in research related to gastroesophageal reflux disease and studies investigating acid secretion mechanisms. -
Potassium Channel Activator
Kaurenoic acid is a diterpene that acts as a potassium channel activator. It exhibits various biological activities, including antibacterial, anti-inflammatory, anticonvulsant, analgesic, and aortic vasodilating effects. This compound is primarily utilized in research related to neuroprotection, cardiovascular health, and the modulation of ion channel activity. -
Calcium Channel Agonist
(2R,3R)-Butane-2,3-diol functions as a reversible agonist of lanthanum-sensitive calcium channels in bacteria, specifically Escherichia coli, with an EC50 of approximately 25 mM. This compound interacts with calcium channel proteins, promoting channel opening and facilitating extracellular calcium influx, which leads to intracellular calcium transients. Such activity plays a crucial role in regulating bacterial physiological processes, including growth, metabolism, and signal transduction. Additionally, (2R,3R)-Butane-2,3-diol is valuable for investigating bacterial-host cell signaling dynamics and studying conditions like lactose intolerance and other related gastrointestinal disorders.
