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
RSC-1255 is a potent and selective inhibitor of Vacuolar H⁺-ATPase (V-ATPase), demonstrating a binding affinity with a Kd of 23 nM. This compound exhibits preferential cytotoxicity towards KRAS-mutant cancer cells, particularly those harboring KRASG13D and KRASG12V mutations. RSC-1255 effectively induces apoptosis while inhibiting lysosomal acidification, autophagy, and macropinocytosis. It serves as a valuable tool for researching KRAS-driven lung and colon cancers. -
ATPase Inhibitor
ATPase-IN-3 is an ATPase inhibitor that demonstrates gastroprotective effects in models of ethanol-induced gastric ulcers. Its mechanism of action involves the modulation of anti-apoptotic pathways through the upregulation of BCL-2 and the activation of tumor suppressor protein P53. This compound is valuable for research applications aimed at investigating gastric ulcer pathophysiology and potential therapeutic interventions. -
Apoptosis Inducer
Rabeprazole-d4 is a deuterated derivative of Rabeprazole, primarily acting as an apoptosis inducer through its irreversible inhibition of gastric H+/K+-ATPase. This second-generation proton pump inhibitor also functions as a uridine nucleoside ribohydrolase (UNH) inhibitor with an IC50 of 0.3 μM. Rabeprazole-d4 is valuable for research focused on gastric ulcerations and gastroesophageal reflux diseases, facilitating studies on its mechanisms of action and therapeutic potential. -
Calcium Antagonist
Cycleanine is a potent vascular-selective calcium antagonist known for its analgesic, muscle relaxant, and anti-inflammatory properties. This compound exhibits potential anti-ovarian cancer effects by modulating the apoptosis pathway, making it a valuable tool for research in oncology and pain management. Its calcium-blocking mechanism allows for further exploration into vascular functions and related biological systems. -
MDR Reversal Agent
Hydrocinchonine is a multidrug resistance (MDR) reversal agent that functions primarily by inhibiting the activity and expression of P-glycoprotein (P-gp). This inhibition plays a critical role in overcoming drug resistance in cancer treatment. Hydrocinchonine has demonstrated a synergistic apoptotic effect when combined with Paclitaxel in MES-SA/DX5 cells, making it a valuable tool for research aimed at addressing drug-resistant gynecological malignancies, such as uterine sarcoma. -
Calcium Channel Antagonist
Benidipine is a potent orally active calcium channel antagonist. It exhibits anti-apoptotic effects in ischemic/reperfused myocardial cells and enhances the activity of endothelial cell-type nitric oxide synthase. Additionally, Benidipine has been shown to improve coronary circulation in hypertensive rat models, making it valuable for research on cardiovascular health and related disorders. -
P-gp Inhibitor
RMS3 is a tetrandrine analogue that functions as a potent inhibitor of P-glycoprotein (P-gp). This compound exhibits significant antiproliferative and cytotoxic effects on various cancer cell lines. Notably, RMS3 induces PARP cleavage, which is indicative of cells undergoing apoptosis. Its strong anticancer properties make RMS3 a valuable tool for cancer research and therapeutic studies. -
P-gp Inhibitor
RMS5 is a potent P-glycoprotein (P-gp) inhibitor, derived from a tetrandrine analogue. It exhibits significant antiproliferative and cytotoxic effects on cancer cells, contributing to its strong anticancer properties. Additionally, RMS5 has been observed to reduce the expression of anti-apoptotic Bcl-2 family proteins Bcl-XL and Mcl-1 while inducing PARP cleavage, a hallmark of apoptosis. This compound is valuable for research applications focusing on cancer therapeutics and the modulation of multidrug resistance. -
Stable Isotope
Capsaicin-d3 is a deuterated form of Capsaicin, a well-known TRPV1 agonist derived from chili peppers. This stable isotope allows for precise tracking and analysis in various research applications. Capsaicin-d3 has been implicated in studies exploring analgesic effects for neurological disorders, as well as its potential antioxidant, anti-inflammatory, and anti-cancer properties. Its use in research facilitates a better understanding of pain pathways and the therapeutic potential of capsaicin-related compounds. -
Stable Isotope
Pantoprazole-d6 is a deuterated form of Pantoprazole, a potent proton pump inhibitor (PPI) targeting H+/K+-ATPase with an IC50 of 6.8 μM. This stable isotope is primarily utilized in pharmacokinetic studies and metabolic investigations. Pantoprazole exhibits significant anti-secretory and anti-ulcer activities, enhancing pH stability while demonstrating the potential to improve tumor growth delay when combined with Doxorubicin. -
Antiarrhythmic Agent
Quinidine gluconic acid is an antiarrhythmic agent primarily targeting potassium channels, exhibiting an IC50 of 19.9 μM. This compound is a potent, orally active inhibitor of cytochrome P450 enzymes and has been shown to induce apoptosis in certain cell types. Quinidine gluconic acid is utilized in research related to cardiac arrhythmias as well as malaria studies, providing valuable insights into these complex biological processes. -
P-gp Inhibitor
(R)-OY-101 is an orally active and selective inhibitor of P-glycoprotein (P-gp). This compound enhances the sensitivity of tumors to anticancer agents by reversing drug resistance and promoting apoptosis. It has valuable applications in cancer research, particularly in studies focused on overcoming multidrug resistance and improving therapeutic efficacy. -
Na+/K+ ATPase Activator
Oleic acid sodium, also known as sodium oleate, is a sodium salt of the monounsaturated fatty acid oleic acid. It functions as an activator of Na+/K+ ATPase, which is essential for maintaining ion gradients across cell membranes. This compound has significant implications in various biological research applications, particularly in studies involving membrane function and cellular signaling pathways. -
SERT/NET Inhibitor
Amitriptyline is a tricyclic antidepressant that primarily inhibits the serotonin transporter (SERT) and norepinephrine transporter (NET), enhancing synaptic levels of serotonin and norepinephrine. With a Ki value of 3.45 nM for SERT and 13.3 nM for NET, Amitriptyline demonstrates significant antidepressant activity. Additionally, it exhibits agonistic properties at α2A adrenergic and TrkA/TrkB receptors, contributing to its analgesic and neurotrophic effects. Furthermore, Amitriptyline interacts with various receptors, including muscarinic cholinergic and H1 receptors, which may lead to a variety of side effects, while its ability to block sodium channels and hERG potassium channels raises concerns regarding cardiotoxicity. -
P-Glycoprotein Inhibitor
(R)-Verapamil hydrochloride is an orally active P-Glycoprotein inhibitor that effectively blocks MRP1-mediated transport. This compound induces apoptosis and inhibits L-type calcium channels, including BZPcc, DHPcc, and PLLcc. Additionally, (R)-Verapamil hydrochloride demonstrates potential anti-septic shock and anti-diabetic effects, making it suitable for a range of research applications in cellular signaling and drug transport studies. -
Nucleotide Analogue
Uridine 5'-monophosphate disodium salt is a nucleotide analogue that activates mitochondrial ATP-dependent potassium channels, providing cardioprotective effects. This compound facilitates the synthesis of CDP-choline and induces apoptosis in intestinal epithelial cells, supporting gut development and reducing the incidence of diarrhea. It serves as a valuable tool for studies related to cardiac health and gastrointestinal function. -
NF-κB Expression Reducer, ERK 1/2 Activator, Beta-Adrenergic Receptor Modulator, Calcium Channel Inhibitor
Eupatorin is a flavonoid that functions primarily as an NF-κB expression reducer and an ERK 1/2 activator, while also modulating beta-adrenergic receptors and inhibiting calcium channels. It demonstrates significant antiproliferative and vasodilatory effects, inducing apoptosis and causing G2/M phase cell cycle arrest, alongside reactive oxygen species (ROS) production. Eupatorin has been shown to impact inflammatory mediators and calcium signaling pathways, making it relevant for research in breast cancer, hypertension, and leukemia. Metabolized by CYP1A1 and other CYP1 enzymes, Eupatorin yields bioactive metabolites that maintain antiproliferative properties. -
Calcium Channel Modulator
4-Bromo A23187 is a halogenated analog of the selective calcium ionophore A-23187, acting as a calcium channel modulator. This compound facilitates the transport of calcium ions across cellular membranes, leading to increased intracellular calcium levels. It has demonstrated efficacy in inducing apoptosis in various cell types, including HL-60 cells, and is useful for research applications related to calcium-mediated signaling pathways and cell death mechanisms. -
PP Inhibitor
Pantoprazole sodium hydrate is a potent proton pump inhibitor (PPI) that targets the H+/K+-ATPase enzyme. With an IC50 value of 6.8 μM, it exhibits significant anti-secretory and anti-ulcer properties. This compound has been demonstrated to enhance tumor growth delay when used in combination with Doxorubicin, making it a valuable reagent for studies involving cancer treatment and gastrointestinal disorders. -
Calcium Sensitiser
OR-1896 is a potent calcium sensitizer and active metabolite of Levosimendan, primarily targeting phosphodiesterase (PDE) III isoforms. It exhibits significant vasodilatory effects and can activate ATP-sensitive potassium channels, enhancing calcium sensitivity. OR-1896 has been shown to reduce cardiomyocyte apoptosis, alleviate cardiac remodeling, and mitigate myocardial inflammation, making it valuable for research in cardiovascular disease therapies. -
F0F1-ATPase Inhibitor
Apoptolidin is a polyketide compound that selectively inhibits the mitochondrial F0F1-ATPase. It has been demonstrated to induce apoptotic cell death specifically in cells transformed with adenovirus type 12 oncogenes, such as ElA, with an IC50 of 10-17 ng/ml. Apoptolidin serves as a valuable tool for studying apoptotic mechanisms and mitochondrial function in cancer research. -
Kv2.1 Inhibitor
Kv2.1-IN-1 is a selective inhibitor of the Kv2.1 potassium channel, demonstrating a potent inhibitory activity with an IC50 of 0.07 μM. It exhibits over 130-fold selectivity against other potassium, sodium, and calcium channels. Kv2.1-IN-1 has been shown to reduce H2O2-induced apoptosis in HEK293 cells and provides significant neuroprotective effects in models of middle cerebral artery occlusion (MCAO) in rats. This compound is useful for research into ischemic stroke and related neurological conditions. -
Potassium Binder
Patiromer is a selective, non-absorbable intestinal potassium binder that targets potassium ions through a reversible exchange with calcium ions. It effectively lowers serum potassium levels while promoting fecal potassium excretion and reducing serum aldosterone levels. Patiromer is utilized in research on hyperkalemia associated with conditions such as chronic kidney disease, diabetes, and heart failure, and is particularly beneficial in studies aimed at enhancing the efficacy of renin-angiotensin-aldosterone system inhibitor (RAASi) therapies. -
Histamine H1 Receptor/TRPV1 Inhibitor
Dexbrompheniramine is a dual inhibitor of the histamine H1 receptor and the TRPV1 receptor, enabling it to effectively cross the blood-brain barrier. It functions by blocking H1 receptor activity and inhibiting TRPV1-mediated calcium responses in a dose-dependent manner, including responses triggered by Capsaicin. Research indicates that Dexbrompheniramine, when combined with Cimetidine, can mitigate drinking behavior induced by histamine and sham feeding, while it alone does not induce thirst. This compound is valuable for investigating the pathophysiology of chronic cough and related disorders. -
Stable Isotope
Uridine 5'-monophosphate-13C9,15N2 dilithium is a stable isotope-labeled form of uridine 5'-monophosphate, incorporating both 13C and 15N isotopes. This compound acts as an orally active mitochondrial ATP-dependent potassium channel activator, demonstrating cardioprotective effects. Additionally, uridine 5'-monophosphate promotes the synthesis of CDP-choline and induces apoptosis in intestinal epithelial cells, making it valuable for research in gut development and in studies related to gastrointestinal health. -
Stable Isotope
Rabeprazole-d3 sodium is a deuterium-labeled form of the second-generation proton pump inhibitor, Rabeprazole sodium, which irreversibly inhibits the gastric H+/K+-ATPase. This compound has been shown to induce apoptosis and acts as an uridine nucleoside ribohydrolase (UNH) inhibitor with an IC50 value of 0.3 μM. Rabeprazole-d3 sodium is utilized in research involving gastric ulcerations and gastroesophageal reflux disorders. -
Stable Isotope
Pantoprazole-d8 is a deuterium-labeled form of Pantoprazole, a potent proton pump inhibitor (PPI) that targets H+/K+-ATPase with an IC50 of 6.8 μM. This compound exhibits significant anti-secretory and anti-ulcer activities, enhancing gastric pH stability. Research applications include investigating the pharmacokinetics of Pantoprazole and its potential synergistic effects with other chemotherapeutic agents, such as Doxorubicin, in tumor growth modulation. -
TRPV1 Antagonist
DWP-05195 is a TRPV1 antagonist that inhibits pain signal transduction, providing research applications in pain management studies. Additionally, DWP-05195 induces endoplasmic reticulum (ER) stress-dependent apoptosis in human ovarian cancer cells, mediated by the ROS-p38-CHOP signaling pathway. This compound may be useful for investigating both nociceptive mechanisms and potential therapeutic strategies for ovarian cancer. -
Stable Isotope
Rabeprazole-13C,d3 is a deuterated form of Rabeprazole, a second-generation proton pump inhibitor (PPI) that irreversibly inhibits gastric H+/K+-ATPase. This compound is known to induce apoptosis and has been identified as an inhibitor of uridine nucleoside ribohydrolase (UNH) with an IC50 value of 0.3 μM. Rabeprazole-13C,d3 is utilized in research focused on gastric ulcerations and gastroesophageal reflux disease, facilitating the study of drug metabolism and action in biological systems. -
Stable Isotope
Pantoprazole-d3 is a deuterium-labeled form of Pantoprazole, a potent proton pump inhibitor (PPI) that selectively targets the H+/K+-ATPase enzyme, exhibiting an IC50 of 6.8 μM. This compound enhances gastric pH stability and demonstrates significant anti-secretory and anti-ulcer properties. It is utilized in research to study gastric acid secretion mechanisms and to investigate potential synergistic effects with chemotherapeutic agents, such as Doxorubicin, in cancer treatment. -
Estrogen Receptor Agonist, Voltage-Gated Sodium Channel Blocker, PI3K-AKT/JNK Signaling Modulator,
Propylparaben sodium acts as a weak estrogen receptor agonist and serves as a voltage-gated sodium channel blocker, while also modulating the PI3K-AKT and JNK signaling pathways. It is known to induce oxidative stress, affecting the estrous cycle and hormone levels, as well as ovarian reserve function. Propylparaben sodium can inhibit the growth of antral follicles and influence the accumulation of steroid hormones in follicle culture media. This compound is suitable for research related to ovarian aging and myocardial ischemia-reperfusion injury. -
Antiarrhythmic Agent
Quinidine sulfate is an antiarrhythmic agent that primarily targets cardiac ion channels, particularly potassium channels. It exhibits potent K+ channel blocking activity with an IC50 of 19.9 μM and has been shown to induce apoptosis in various cell types. Additionally, quinidine sulfate is utilized in malaria research, making it valuable for studies related to both cardiovascular and infectious diseases. -
Antiarrhythmic Agent
Quinidine polygalacturonate is an antiarrhythmic agent that primarily targets potassium channels, exhibiting an IC50 of 19.9 μM. It also functions as a selective inhibitor of cytochrome P450db and has the capability to induce apoptosis. This compound is particularly useful in research focused on cardiac arrhythmias and malaria studies, making it a valuable reagent for pharmacological investigations. -
Vasodilator
KMUP-1 is a xanthine derivative that acts as a vasodilator through the inhibition of phosphodiesterase (PDE) and activation of soluble guanylyl cyclase (sGC). It stimulates the nitric oxide/sGC/cyclic GMP signaling pathway and facilitates the opening of potassium channels. Additionally, KMUP-1 has been shown to reduce ischemia-induced cardiomyocyte apoptosis. This compound is relevant for studies in cardiovascular health and anti-inflammatory research. -
P-glycoprotein Inhibitor
P-gp inhibitor 22 is a potent inhibitor of P-glycoprotein (P-gp), effectively blocking its efflux function. This compound has been shown to induce apoptosis and promote the accumulation of MCF-7/ADR cells in the S phase of the cell cycle. Its ability to inhibit P-gp makes it relevant in studies focused on multidrug resistance and cancer therapeutics. -
Potassium Channel Inhibitor
DPO-1 is a selective inhibitor of Kv1.5 and Kv1.3 potassium channels (EC50 = 3.1 μM) with notable immunomodulatory and anti-inflammatory properties. It effectively reduces Kv1.3 current density, diminishes Ca2+ influx in calcium-depleted Jurkat cells, and inhibits IL-2 secretion in activated Jurkat cells. Additionally, DPO-1 obstructs uric acid sodium (MSU)-induced NLRP3 inflammasome activation by interfering with Kv1.5-mediated K+ efflux. This reagent is valuable for research into immunological disorders and atrial fibrillation. -
Sodium Channel Inhibitor
Articaine is a selective inhibitor of voltage-gated sodium channels, including rNav1.4, hNav1.7, and rNav1.8, demonstrating an IC50 of 15.8 μM for open-state Na+ channels. It effectively blocks Na+ influx, leading to local anesthetic effects and interruption of nerve impulse conduction. Additionally, Articaine exhibits anti-inflammatory properties by inhibiting NF-κB activation and the NLRP3 inflammasome pathway. This compound is valuable for research in dental anesthesia and inflammatory-related conditions, such as acute kidney injury. -
CO Donor
Tricarbonyldichlororuthenium(II) dimer serves as a carbon monoxide (CO) donor, facilitating various biological processes. This compound demonstrates notable anti-inflammatory and antioxidant properties, in addition to its protective effects on gastric mucosa. Furthermore, Tricarbonyldichlororuthenium(II) dimer exhibits CO-independent effects on several potassium channels, highlighting its significance in cellular physiology and potential therapeutic applications. -
NAAA Inhibitor
AM9053 is a selective and slowly reversible inhibitor of N-acyl ethanolamine acid amidease (NAAA) with an IC50 of 30 nM. It shows limited impact on FAAH activity (IC50 > 100 nM). AM9053 demonstrates significant anti-proliferative effects on colorectal cancer cells through the activation of PPAR-α and TRPV1-dependent pathways, leading to S-phase cell cycle arrest. Additionally, it alleviates intestinal fibrosis by modulating macrophage activity and inhibiting the IL-23 signaling pathway, resulting in increased levels of N-acylethanolamines, particularly palmitoylethanolamide (PEA) and oleoylethanolamide (OEA). AM9053 is valuable for research into colorectal cancer and intestinal fibrosis. -
ABCG2/BCRP Inhibitor
Triclabendazole sulfoxide is an ABCG2/BCRP inhibitor that serves as the primary plasma metabolite of Triclabendazole. This compound demonstrates significant anti-parasitic activity and is useful in research applications focusing on the modulation of drug transport mechanisms in cellular assays. It contributes to studies investigating the role of ABCG2/BCRP in drug resistance and pharmacokinetics.
