Catalog No.
Product Name
Application
Product Information
Citations
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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. -
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. -
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. -
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. -
Aortic Vasodilator
KMUP-4, a xanthine derivative, primarily acts as an aortic vasodilator by enhancing cyclic guanosine monophosphate (cGMP) levels. It promotes aortic relaxation through both endothelium-dependent and independent pathways by inhibiting phosphodiesterases (PDEs) and activating potassium channels, which also increases cyclic adenosine monophosphate (cAMP). KMUP-4 is a valuable reagent for research on cardiovascular diseases, providing insights into vascular relaxation mechanisms and potential therapeutic targets. -
PDE4 Inhibitor
L-869298 is a potent and selective inhibitor of phosphodiesterase 4 (PDE4), demonstrating an IC50 value of 0.5 nM for the PDE4A isoform. This compound exhibits minimal activity against the hERG potassium channel, making it a valuable tool for studies focused on inflammation, neurodegeneration, and other PDE4-related pathways. Its specificity and efficacy make it a suitable candidate for research applications in therapeutic development targeting PDE4-mediated signaling. -
Potassium-competitive Acid Blocker
KFP-H008 is an orally active potassium-competitive acid blocker that targets H+-K+-ATPase to inhibit gastric acid secretion. This compound has shown efficacy in reducing ethanol-induced gastric ulcer index and decreasing malonaldehyde levels, along with the expression of pro-inflammatory cytokines in vivo. KFP-H008 also downregulates p-p38 MAPK and p65 NF-κB expression, demonstrating its potential in mitigating gastric inflammation. This reagent is valuable for research into acid-related diseases, including gastric ulcers and gastric epithelial cell damage. -
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. -
Kir6.2/SUR inhibitor
Glimepiride is a potent Kir6.2/SUR inhibitor with IC50 of 3.0 nM, 5.4 nM, and 7.3 nM for SUR1, SUR2A and SUR2B, used in the treatment of type 2 diabetes mellitus. - Hydralazine hydrochloride is a hydrochloride salt of hydralazine (Apresoline) that is a direct-acting smooth muscle relaxant with an IC50 of 1.9 mM.
- Minoxidil (U-10858) is a selective ATP dependent K+ (Kir6) channel activator.
- Nateglinide(Starlix) is an insulin secretagog agent that lowers blood glucose levels by stimulating insulin secretion from the pancreas.
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Potassium Channel inhibitor
Repaglinide is a potent short-acting insulin secretagogue that acts by closing ATP-sensitive potassium (KATP) channels in the plasma membrane of the pancreatic beta cell. -
potassium currents blocker
Gliclazide is used as an antidiabetic. It is a whole-cell beta-cell ATP-sensitive potassium currents blocker with an IC50 of 184 nM.
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Potassium Channel inhibitor
Acecainide, also known as N-acetylprocainamide and ASL 601, is the N-acetylated metabolite of procainamide. Acecainide is a Class III antiarrhythmic agent. It can be given either intravenously or orally, and is eliminated primarily by renal excretion. -
Serotonergic Receptor Antagonist
Hymenidin is a natural antagonist of serotonergic receptors, exhibiting significant inhibitory effects on voltage-gated potassium channels. This compound demonstrates the ability to induce apoptosis in cancer cells, making it a valuable tool for research in cancer biology and therapeutics targeting serotonergic signaling pathways. Its dual action on ion channels and receptor antagonism positions Hymenidin as a noteworthy reagent for exploring complex cellular mechanisms in neurobiology and oncology. -
K+ Channels Activator
1-EBIO is an activator of Ca2+-sensitive K+ channels, playing a crucial role in the modulation of membrane potential and cellular excitability. This compound is utilized in research to investigate the physiological functions and pathophysiological roles of K+ channels, contributing to a deeper understanding of cellular signaling processes and potential therapeutic targets in various diseases. -
Anti-microbial Agent/Kir3.2 Blocker
3,6-Diaminoacridine hemisulfate is an acridine compound that functions primarily as a broad-spectrum antimicrobial agent and a Kir3.2 potassium channel blocker. Its mechanism involves insertion into bacterial DNA, thereby disrupting replication and transcription, which ultimately leads to bacterial lysis. Additionally, this compound is utilized in research to investigate the neurological phenotype associated with Down syndrome. Due to its ability to penetrate the stratum corneum and accumulate in the cell nucleus, prolonged exposure warrants caution due to potential oncogenic effects. -
Stable Isotope
Terfenadine-d3 is the deuterated form of Terfenadine, which primarily targets the hERG potassium channel as a potent open-channel blocker with an IC50 of 204 nM. As an H1 histamine receptor antagonist, Terfenadine-d3 demonstrates significant biological activity by inducing apoptosis in melanoma cells through the modulation of calcium homeostasis. Its mechanism includes the generation of reactive oxygen species (ROS) and the subsequent activation of caspases -4, -2, and -9, making it valuable for research in cancer biology and apoptosis pathways. -
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. -
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. -
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. -
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. -
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. -
HDAC inhibitor
HL23 is a histone deacetylase (HDAC) inhibitor with demonstrated efficacy against hepatocellular carcinoma (HCC). It enhances acetylation at the TXNIP promoter, leading to upregulation of TXNIP expression and modulation of potassium channel activity, ultimately inducing TXNIP-dependent potassium deprivation. HL23 effectively suppresses HCC progression and metastasis, and exhibits a synergistic antitumor effect when combined with Sorafenib, outperforming the combination of Sorafenib and Vorinostat in preclinical models. -
TNFα/IL-2 Inhibitor
Immuno modulator-1 is a potent inhibitor of TNFα and IL-2, displaying IC50 values of 4.7 nM and 26 nM, respectively, in human peripheral blood mononuclear cells (hPBMC). This compound is valuable for investigating immune response modulation and inflammatory pathways. Additionally, Immuno modulator-1 demonstrates a hERG potassium channel blocking effect, exhibiting a 20% inhibitory percentage at a concentration of 3 μM, making it relevant for studies involving cardiac safety profiles. -
Potassium Channel Inhibitor
Endoxifen Z-isomer hydrochloride is a selective potassium channel inhibitor that acts as a potent metabolite of Tamoxifen, exhibiting over 100-fold increased potency compared to its parent compound. This compound effectively inhibits PKCβ1 kinase activity, leading to decreased phosphorylation of AKT at Ser473 and its substrates, which ultimately promotes apoptosis. Endoxifen Z-isomer hydrochloride demonstrates significant anticancer effects, particularly against hormone-resistant metastatic breast cancer, making it a valuable reagent for cancer research applications. -
Stable Isotope
Trimebutine-d5 fumarate is a deuterium-labeled derivative of Trimebutine fumarate, functioning primarily as a multi-target inhibitor and opioid receptor agonist. This compound exhibits key biological activities, including the inhibition of L-type Ca2+ channels and large-conductance calcium-activated potassium channels (BKCa), which regulate calcium influx and potassium efflux. Additionally, Trimebutine-d5 fumarate targets Toll-like receptors, modulating inflammatory signaling pathways, and promotes apoptosis in tumor cells via the AKT/ERK pathway. Its applications are particularly relevant in the study of gastrointestinal disorders, including irritable bowel syndrome (IBS), due to its ability to inhibit excessive smooth muscle contraction. -
Progranulin secretion Activator
Progranulin modulator-1 is a selective activator of progranulin (PGRN) secretion. It significantly increases PGRN levels in BV-2 cells and exhibits low cytotoxicity with an EC50 value of 83 nM for PGRN. Additionally, Progranulin modulator-1 inhibits the hERG potassium channel with an IC50 of 3100 nM, making it a valuable tool for research on neuroinflammation and associated neurodegenerative disorders. -
Anti-inflammatory Agent
Siaresinolic acid is an anti-inflammatory compound derived from the leaves of Sabicea grisea. It exhibits significant antinociceptive properties by modulating ATP-dependent potassium channels and inhibiting the influx of leukocytes, plasma leakage, and the production of pro-inflammatory mediators such as TNF-α and IL-1β. Importantly, Siaresinolic acid demonstrates a lack of cytotoxicity in murine macrophages and does not affect locomotor activity even at elevated doses. This compound is suitable for research applications involving pleurisy and pain management. -
ASK1 Inhibitor
ASK1-IN-11 is a potent inhibitor of apoptosis signal-regulating kinase 1 (ASK1), exhibiting an IC50 of less than 200 nM. This compound also demonstrates inhibitory effects on TNF-α, MYLK/MLCK kinases, and hERG potassium channels. The primary research applications of ASK1-IN-11 include investigations into inflammation-related pathways. -
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. -
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. -
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. -
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. -
TREK-1 Channel Blocker
Spadin is a potent TREK-1 channel blocker with an IC50 value of 10 nM. This natural peptide, derived from a propeptide released into the bloodstream, enhances 5-HT neurotransmission in the dorsal raphe nucleus of mice, promoting hippocampal CREB activation and neurogenesis. Spadin is valuable for research applications targeting antidepressant mechanisms and neuroplasticity. -
Stable Isotope
Chlorpromazine-d6 hydrochloride is a deuterated derivative of Chlorpromazine, primarily functioning as a dopamine receptor antagonist. This stable isotope is utilized in biochemical and pharmacological research to explore the interactions and mechanisms of action of antipsychotic agents. Its ability to inhibit serotonin receptors, potassium channels, and sodium channels makes it valuable for studying neuropharmacology and drug metabolism. -
Potassium Channel Inhibitor
Naluzotan hydrochloride is a selective potassium channel inhibitor that primarily functions as an amidosulfonamide 5-HT1A agonist, exhibiting an IC50 of approximately 20 nM and a Ki value of 5.1 nM. This compound demonstrates notable activity in modulating neurotransmitter pathways, making it a valuable tool for research into anxiety and depression treatments. Additionally, naluzotan hydrochloride acts as a weak hERG K+ channel blocker with an IC50 of 3800 nM, highlighting its potential relevance in cardiac safety assessments.
